This list of chemotherapeutic agents covers the cancers each drug is used for, as well as the recommended dosage and possible toxicities of the therapy.
Use: Metastatic castration-resistant prostate cancer
Dosage: 1,000 mg PO daily on an empty stomach in combination with prednisone 5 mg orally twice daily
Toxicities may include: Fatigue, joint swelling or discomfort, hypokalemia, edema, hot flushes, diarrhea, urinary tract infection, cough, hypertension, arrhythmia, urinary frequency, nocturia, dyspepsia, upper respiratory tract infection, increases in liver enzyme levels, adrenocortical insufficiency
Use: Metastatic breast cancer as second line treatment, locally advanced or metastatic non-small–cell lung cancer (NSCLC), metastatic adenocarcinoma of the pancreas in combination with gemcitabine.
Dosage: For patients with metastatic breast cancer, 260 mg/m2 IV every 3 weeks; for those with NSCLC, 100 mg/m2 IV on days 1,8, and 15 of a 21-day cycle; for patients with pancreatic cancer, 125 mg/m2 IV on days 1,8, and 15 of a 28-day cycle
Toxicities may include: Bone marrow depression, sensory and peripheral neuropathy, arthralgia/myalgia, asthenia, abnormal electrocardiogram, alopecia, fatigue, nausea
Use: Chemotherapy-refractory B-cell chronic lymphocytic leukemia
Dosage: Premedication with acetaminophen and diphenhydramine recommended prior to first dose and dose escalations. Rapid daily-dose escalation, until tolerated, from 3 mg/d, and then 10 mg/d, to the recommended maintenance dose of 30 mg IV over 120 minutes, three times per week on alternate days for up to 12 weeks
Toxicities may include: Pancytopenia, infusion reaction, opportunistic infections, skin rash, nausea/vomiting, insomnia
Use: Ovarian cancer
Dosage: 260 mg/m2 PO, divided in four doses for 14–21 days of a 28-day regimen
Toxicities may include: Nausea and vomiting, bone marrow depression, neuropathies, neurotoxicities
Use: Peripheral T-cell lymphoma
Dosage: 1,000 mg/m2 IV over 30 minutes on days 1–5 of a 21-day cycle
Toxicites may include: Nausea, fatigue, fevers, anemia, and vomiting
Use: Chronic lymphocytic leukemia, B-cell non-Hodgkin lymphoma (relapsed)
Dosage: 100 mg/m2 IV on day 1 and day 2 of a 28-day cycle, up to 6 cycles
Toxicities may include: Bone marrow depression, fever, nausea, and vomiting
Use: Breast cancer, colorectal cancer, non–small-cell lung cancer, renal cell carcinoma, glioblastoma (relapse), cervical cancer, epithelial ovarian, fallopian tube, primary peritoneal cancer.
Dosage: 5–15 mg/kg/wk IV every 14–21 days
Toxicities may include: Asthenia, headache, epistaxis, proteinuria, gastrointestinal perforations/wound-healing complications, hypertension/hypertensive crisis; hemorrhage, thromboembolic event, ovarian failure, osteonecrosis of the jaw, posterior reversible encephalopathy syndrome, infusion reactions, embryo-fetal toxicity, rhinitis, taste alterations, dry skin, lacrimation disorder, back pain, exfoliative dermatitis
Use: Philadelphia chromosome–negative (Ph−) relapsed or refractory B-cell acute lymphoblastic leukemia
Dosage: Cycle one: 9 μg/d as a continuous infusion on days 1–7, then 28 μg/d as a continuous infusion on days 8–28. Subsequent cycles: 28 μg/d as a continuous infusion on days 1–28
Toxicities may include: cytokine release syndrome, neurologic toxicities, pyrexia, headache, peripheral edema, febrile neutropenia, nausea, hypokalemia, tremor, rash, constipation
Use: Testicular cancer, Hodgkin lymphoma; reticulum cell sarcoma (histiocytic lymphoma); lymphosarcoma; squamous cell cancer of the head and neck, skin, cervix, vulva, and penis
Dosage: 10–20 U/m2 given IV, IM, or SC weekly or twice weekly; maximum total dose, 400 U; a 2-U test dose should be given because of a possible anaphylactoid reaction
Toxicities may include: Pneumonitis and pulmonary fibrosis, fever and allergic reactions, anaphylaxis, hyperpigmentation, Raynaud phenomenon, alopecia
Use: Multiple myeloma
Dosage: 1.3 mg/m2 on days 1, 4, 8, and 11 every 3 weeks
Toxicities may include: Diarrhea, peripheral neuropathy, asthenia, fever, anorexia, Mantle cell lymphoma, nausea and vomiting, rash, headache, thrombocytopenia
Use: Hodgkin lymphoma after failure of autologous stem cell transplant (ASCT) or after failure of at least two prior multiagent chemotherapy regimens in patients who are not candidates for ASCT; or treatment of patients with systemic anaplastic large-cell lymphoma after failure of at least one prior multi-agent chemotherapy regimen.
Dosage: 1.8 mg/kg IV infusion over 30 minutes every 3 weeks (maximum of 16 cycles)
Toxicities may include: Neutropenia, peripheral sensory neuropathy, abdominal pain, fatigue, nausea, anemia, upper respiratory tract infection, diarrhea, pyrexia, rash, thrombocytopenia, cough, vomiting
Use: Chronic myeloid leukemia, bone marrow transplantation for refractory leukemia, lymphomas
Dosage: 2–8 mg PO daily for remission induction; adjust dosage to white blood cell (WBC) count; 1–3 mg PO daily for maintenance; withhold induction if WBC count is < 15,000/µL; resume therapy when WBC count is > 50,000/µL
Toxicities may include: Bone marrow depression, pulmonary fibrosis, aplastic anemia, amenorrhea, gynecomastia, skin hyperpigmentation
Use: Hormone-refractory metastatic prostate cancer previously treated with docetaxel regimens
Dosage: 25 mg/m2 IV every 3 weeks in combination with prednisone at 10 mg PO daily throughout cabazitaxel treatment. Premedicate 30 minutes before each dose with antihistamine, corticosteroid, and H2 antagonist.
Toxicities may include: Febrile neutropenia (primary prophylaxis with granulocyte colony-stimulating factor should be considered in high-risk patients), nausea, vomiting, diarrhea, renal failure, hypersensitivity reactions
Use: Breast cancer (relapsed), colorectal cancer, and other gastrointestinal malignancies
Dosage: 1,250 mg/m2 bid PO with food (2 weeks on drug, 1 week of rest)
Toxicities may include: Diarrhea, stomatitis, nausea and vomiting, fatigue, hand-foot syndrome, bone marrow depression (minimal)
Use: Ovarian cancer; endometrial, head and neck, lung, testicular, and breast cancers; relapsed acute leukemia, non-Hodgkin lymphoma
Dosage: Single agent: 360 mg/m2 IV every 4 weeks; combination: 300 mg/m2 IV every 4 weeks; Calvert formula: Total dose (mg) = Target area under the curve × [glomerular filtration rate (GFR) + 25]
Toxicities may include: Bone marrow depression, nausea and vomiting, peripheral neuropathy, ototoxicity
Total carboplatin dose calculation based on serum creatinine levels measured by isotope dilution mass spectrometry using the Calvert formula may result in overestimation of the GFR in some patients with normal renal function, and therefore increased drug-related toxicity. When actual GFR measurements are made to assess renal function, carboplatin can be safely dosed as outlined in the package insert.
Use: Brain tumor, multiple myeloma, Hodgkin lymphoma, non-Hodgkin lymphoma, melanoma, bone marrow transplant for patients with refractory solid tumors and lymphomas
Dosage: 150–200 mg/m2 IV every 6–8 weeks
Toxicities may include: Delayed bone marrow depression, nausea and vomiting, reversible hepatotoxicity, local phlebitis, pulmonary and renal damage (with high-dose therapy)
Use: Patients with ALK-positive metastatic non–small-cell lung cancer who progress on, crizotinib or cannot tolerate it
Dosage: 750 mg PO once a day
Toxicites may include: Interstitial lung disease, QT interval prolongation, hyperglycemia, bradycardia, embryo-fetal toxicity, diarrhea, nausea, transaminitis, vomiting, abdominal pain, fatigue, decreased appetite, constipation
Use: KRAS wild-type colorectal cancer, head and neck cancer
Dosage: Loading dose of 400 mg/m2 IV over 120 min, and 250 mg/m2 IV over 60 min every 7 days, as maintenance
Toxicities may include: Skin rash, infusion reaction, asthenia, diarrhea, nausea, hypomagnesemia
Use: Chronic lymphocytic leukemia, Hodgkin lymphoma, non-Hodgkin lymphoma, ovarian cancer, choriocarcinoma, lymphosarcoma
Dosage: 0.1–0.2 mg/kg PO daily for 3–6 weeks as required (usually 4–10 mg/d) or intermittent 0.4 mg/kg every 3–4 weeks; increase by 0.1 mg/kg until control of disease or toxicity
Toxicities may include: Bone marrow depression, gonadal dysfunction, leukemia, hyperuricemia, pulmonary fibrosis
Use: Testicular, ovarian, bladder, uterine, cervical, and lung cancers, squamous cell cancer of the head and neck, sarcoma, non-Hodgkin lymphoma
Dosage: 50 mg/m2 IV or more every 3 weeks; or 20 mg/m2 IV daily for 4–5 days every 3–4 weeks; hydrate patient vigorously before and after chemotherapy
Toxicities may include: Renal damage, nausea and vomiting, electrolyte disturbance, peripheral neuropathy, bone marrow depression, ototoxicity, radiosensitizer
Use: Hairy-cell leukemia, non-Hodgkin lymphoma, mycosis fungoides, acute myeloid leukemia, chronic myeloid leukemia, chronic lymphocytic leukemia
Dosage: 0.09 mg/kg/d (4 mg/m2/d) by continuous IV infusion for 7 consecutive days
Toxicities may include: Bone marrow depression, febrile episodes, rash, infections, septicemia
Use: Anaplastic lymphoma kinase (ALK)-mutation–positive non–small-cell lung cancer
Dosage: 250 mg orally twice daily
Toxicities may include: Vision disorder, nausea, diarrhea, vomiting, edema, constipation, increased levels of alanine aminotransferase, neutropenia, pneumonitis
Use: Acute myeloid leukemia, acute lymphoblastic leukemia, chronic lymphocytic leukemia, Hodgkin lymphoma, and non-Hodgkin lymphoma, multiple myeloma; mycosis fungoides; neuroblastoma; ovarian and breast cancers; retinoblastoma; lung, testicular, and bladder cancers; sarcoma
Dosage: 40–50 mg/kg IV in divided doses over 2–5 days to start, followed by 10–15 mg/kg IV every 7–10 days; or 3–5 mg/kg IV twice weekly; or 1–5 mg/kg/d PO
Toxicities may include: Bone marrow depression, hemorrhagic cystitis, immunosuppression, alopecia, stomatitis, syndrome of inappropriate antidiuretic hormone secretion (SIADH)
Use: Acute myeloid leukemia (AML), acute lymphoblastic leukemia, chronic myeloid leukemia, non-Hodgkin lymphoma, central nervous system leukemia (intrathecal)
Dosage: Induction therapy for AML: 100 mg/m2/d by continuous IV infusion on days 1–7; or 100 mg/m2 IV every 12 hours on days 1–7; Relapsed ALL: 3 g/m2 IV over 1–3 hours every 12 hours for four doses
Toxicities may include: Bone marrow depression, nausea and vomiting, diarrhea, arachnoiditis (intrathecal), stomatitis, hepatic dysfunction, fever, conjunctivitis, confusion, somnolence, cerebellar toxicity
Use: As monotherapy for patients with unresectable or metastatic melanoma with BRAF V600E mutations or in combination with trametinib
Dosage: 150 mg PO twice a day
Toxicites may include: New primary malignancies, tumor promotion in BRAF wild-type melanoma, hemorrhage, thromboembolism, cardiomyopathy, occular toxicities, fevers, skin rashes and infections, hyperglycemia, embryo-fetal toxicity, hyperkeratosis, headache, arthralgia, alopecia, palmar-plantar erythrodysesthia, night sweats, chills, nausea, vomiting, peripheral edema, decreased appetite, constipation, myalgias
Use: Malignant melanoma, Hodgkin lymphoma (HL), soft-tissue sarcomas, neuroblastoma
Dosage: Melanoma: 2–4.5 mg/kg/d IV for 10 days every 4 weeks; or 250 mg/m2/d IV for 5 days every 3 weeks HL: 375 mg/m2 IV on day 1, repeated every 15 days (single agent); 150 mg/m2/d IV for 5 days every 4 weeks (combination therapy)
Toxicities may include: Bone marrow depression, nausea and vomiting, flu-like syndrome, transient hepatotoxicity, local irritation, facial flushing, alopecia
Use: Testicular cancer, gestational trophoblastic tumors, Wilms tumor, rhabdomyosarcoma, Ewing sarcoma
Dosage: 0.010–0.015 mg/kg IV daily for 5 days every 3 weeks (usual adult dose, 0.5 mg) or 2 mg/m2 IV as a single dose every 3–4 weeks
Toxicities may include: Stomatitis, bone marrow depression, anorexia, nausea and vomiting, diarrhea, alopecia, skin changes, anaphylactoid reaction
Use: Chronic myeloid leukemia (CML), Philadelphia chromosome positive (Ph+) acute lymphoblastic leukemia
Dosage: 140 mg/d (divided doses; 70 mg bid) or 100 mg/d PO (chronic phase CML)
Non-hematologic toxicities may include: Fluid-retention events (eg, pleural effusion); gastrointestinal events (diarrhea, nausea, abdominal pain, and vomiting; and bleeding events).
Hematologic toxicities may include: neutropenia, thrombocytopenia, anemia
Use: Acute myeloid leukemia, acute lymphoblastic leukemia
Dosage: Remission induction: 30–45 mg/m2/d IV for 3 days in combination therapy; total cumulative dose, 550 mg/m²
Toxicities may include: Bone marrow depression, cardiotoxicity, alopecia, nausea and vomiting, diarrhea, stomatitis, fever, dermatitis at previously irradiated sites, red urine, anaphylactoid reaction
Use: Kaposi sarcoma, acute lymphoblastic leukemia, acute myeloid leukemia
Dosage: Liposomal preparation: 40 mg/m2 IV every 2 weeks
Use: Central nervous system leukemia/lymphoma
Dosage: Intrathecal: DepoCyt, 50 mg over 1–5 minutes every 14 days, with dexamethasone, 4 mg PO bid × 5 days
Use: Breast, non–small-cell lung, prostate, ovarian, pancreatic, head and neck, esophagus, stomach, cervical, uterine, and bladder cancers; Kaposi sarcoma
Dosage: 60–100 mg/m2 IV over 1 hour every 21 days or up to 42 mg/m2 IV every week
Toxicities may include: Bone marrow depression, fluid retention, hypersensitivity reaction, paresthesias, rash, alopecia, myalgias
Use: Ovarian cancer (refractory to paclitaxel- and platinum-based regimens), Kaposi sarcoma, breast cancer, multiple myeloma
Dosage: 50 mg/m2 IV every 4 weeks, 20 mg/m2 IV every 3 weeks
Toxicities may include: Bone marrow depression, hand-foot syndrome, infusional reactions
Use: Acute lymphoblastic leukemia, acute myeloid leukemia; breast, ovarian, and bladder cancers; Hodgkin lymphoma and non-Hodgkin lymphoma, small-cell lung cancer, gastric cancer, sarcoma, Wilms tumor, neuroblastoma, and thyroid cancer; soft-tissue and bone sarcomas
Dosage: 60–90 mg/m2 single IV injection every 21 days, 20–30 mg/m2/d IV for 3 days every 3–4 weeks, or 20 mg/m2 IV weekly. Total cumulative dose should be 550 mg/m2; reduce dose for liver dysfunction
Toxicities may include: Bone marrow depression, cardiotoxicity, stomatitis (continuous infusion), alopecia, nausea and vomiting, diarrhea, fever, dermatitis at previously irradiated sites, red urine, anaphylactoid reaction
Use: Breast cancer
Dosage: 100 mg/m2 IV on day 1 or 60 mg/m2 IV on days 1 and 8 in combination therapy
Toxicities may include: Bone marrow depression, cardiotoxicity, stomatitis, alopecia
Use: Breast cancer (relapse)
Dosage: 1.4 mg/m2 on days 1 and 8 every 21 days
Toxicities may include: Neutropenia, anemia, asthenia/fatigue, alopecia, peripheral neuropathy, nausea, constipation
Use: Non–small-cell lung cancer, pancreatic cancer
Dosage: 150 mg/d PO; 100 mg/d PO (pancreatic cancer)
Toxicities may include: Acneiform skin rash, diarrhea, anorexia, fatigue, dyspnea
Use: Prostate, renal cell carcinomas
Dosage: 14 mg/kg/d PO in 3–4 equally divided doses; 300 mg/d IV for 3–4 weeks, followed by 300–450 mg/weeks IV over 3–8 weeks
Toxicities may include: Bone marrow depression, ischemic heart disease, thromboembolism, thrombophlebitis, gynecomastia, nausea and vomiting, hepatotoxicity
Use: Testicular cancer (refractory), small-cell lung cancer, Hodgkin lymphoma, non-Hodgkin lymphoma, acute myeloid leukemia, gestational trophoblastic tumors. (For both indications, etoposide is given with combination therapy and repeated every 3–4 weeks.)
Dosage: Testicular cancer: 50–100 mg/m2/d IV for 5 days or 100 mg/m2/d IV on days 1, 3, and 5; lung cancer: 35–50 mg/m2/d IV for 5 days or 100 mg/m2/d PO for 5 days
Toxicities may include: Bone marrow depression, nausea and vomiting, diarrhea, fever, hypotension (in case of rapid infusion), alopecia, rash, acute myeloid leukemia (late effect)
Use: Renal cell carcinoma (with treatment progression to tyrosine kinase inhibitors), pancreatic neuroendocrine tumors, subependymal giant cell astrocytoma (SEGA)
Dosage: 10 mg/d PO; SEGA: initial dose based on body surface area with subsequent titration to attain trough concentrations of 5–10 ng/mL
Toxicities may include: Stomatitis, infections, asthenia, diarrhea, pneumonitis, dyslipidemia, hyperglycemia, elevated serum creatinine levels
Use: Gastrointestinal (GI) adenocarcinomas metastatic to liver, including oral, pancreatic, biliary, colon, and hepatic cancers; and metastatic breast cancer
Dosage: 0.1–0.6 mg/kg/d over several days via continuous arterial infusion supplying well-defined tumor; treatments given over 1–6 weeks
Toxicities may include: Stomatitis and GI ulcers, bone marrow depression, abdominal pain, nausea and vomiting, diarrhea, liver dysfunction (transient)
Use: Chronic lymphocytic leukemia, acute myeloid leukemia, non-Hodgkin lymphoma (low-grade)
Dosage: 25 mg/m2/d IV over 30 min for 5 days; repeat every 28 days
Toxicities may include: Bone marrow depression, nausea and vomiting, fever, malaise, pulmonary infiltrates, tumor lysis syndrome, central nervous system effects (high dose)
Use: Colon, rectal, stomach, pancreatic, breast, head and neck, renal cell, prostate, and ovarian cancers; squamous cell carcinomas of the esophagus; basal and squamous cell carcinoma of skin (topical); and hepatic cancer (intra-arterial)
Dosage: Loading dose: 300–500 mg/m2; or 12 mg/kg IV daily for 3–5 days, followed by weekly maintenance; maintenance: 10–15 mg/kg IV weekly, as toxicity permits; infusion: 20–25 mg/kg by continuous IV over 24 hours for 4–5 days, every 4 weeks
Toxicities may include: Stomatitis and gastrointestinal ulcers (infusion), bone marrow depression (bolus), diarrhea, nausea and vomiting, esophagitis, angina, cerebellar ataxia, radiosensitizer
Use: Non–small-cell lung cancer
Dosage: 250 mg/d PO
Toxicities may include: Acneiform skin rash, diarrhea, transaminitis, asthenia, nausea/vomiting, interstitial lung disease
Use: Pancreatic, lung, breast, ovarian, and bladder cancers
Dosage: 1,000 mg/m2 IV over 30 minutes, once weekly for up to 7 weeks (or until toxicity necessitates reducing or withholding a dose), followed by 1 week of rest; subsequent cycles: infusions once weekly for 3 consecutive weeks out of every 4 weeks
Toxicities may include: Bone marrow depression, transient fever, flu-like syndrome, skin rash, mild nausea and vomiting
Use: Glioblastoma multiforme
Dosage: Up to 8 in brain cavity created by tumor removal
Toxicities may include: Fever, pain, and abnormal healing
Use: Chronic myeloid leukemia, acute leukemia (emergent treatment), head and neck cancer, ovarian cancer, melanoma, essential thrombocytosis, polycythemia vera
Dosage: Intermittent: 80 mg/kg PO every third day; continuous: 20–30 mg/kg PO daily
Toxicities may include: Bone marrow depression, mild nausea and vomiting, skin rashes, radiosensitivity
Use: CD20+ low grade follicular B-cell non-Hodgkin lymphoma (relapse)
Dosage: Dosimetric step: rituximab at 250 mg/m2 IV, followed by 5 mCi In-111 ibritumomab on day 1; therapeutic step: day 7, 8, or 9 rituximab at 250 mg/m2 IV, followed by 0.4–0.3 mCi/kg Y-90 ibritumomab
Toxicities may include: Myelosuppression, infection, gastrointestinal symptoms, myelodysplastic syndromes/, acute myeloid leukemia
Use: Mantle cell lymphoma (MCL), chronic lymphocytic leukemia (CLL), Waldenström macroglobulinemia (WM)
Dosage: MCL 560 mg PO once a day; CLL, WM: 420 mg PO once a day
Toxicities may include: Hemorrhage, infections, myelosuppression, atrial fibrillation, second primary malignancies, tumor lysis syndrome, embryo-fetal toxicites, diarrhea, fatigue, musculoskeletal pain, bruising, nausea, upper respiratory tract infections, rash
Use: Acute myeloid leukemia, chronic myeloid leukemia (blast phase), acute lymphoblastic leukemia
Dosage: 12 mg/m2/d IV for 3 days every 3 weeks in combination therapy
Toxicities may include: Bone marrow depression, nausea and vomiting, stomatitis, alopecia, cardiotoxicity
Use: Chronic lymphocytic leukemia in combination with rituximab, follicular lymphoma, small lymphocytic lymphoma
Dosage: 150 mg orally twice a day
Toxicities may include: Severe cutaneous reactions, anaphylaxis, neutropenia, embryo-fetal toxicity, diarrhea, pyrexia, fatigue, nausea, cough, pneumonia abdominal pain, chills, and rash
Use: Germ-cell testicular cancer, sarcoma, non-Hodgkin lymphoma, lung cancer
Dosage: 1.2 g/m2/d via slow IV infusion for 5 consecutive days; repeat every 3 weeks; give with mesna
Toxicities may include: Bone marrow depression, hemorrhagic cystitis, confusion, somnolence
Use: Chronic myeloid leukemia (CML), gastrointestinal stromal tumor (GIST), Philadelphia chromosome–positive (Ph+) acute lymphoblastic leukemia, dermatofibrosarcoma protuberans, mastocytosis, myelodysplastic syndromes/myeloproliferative disorders
Dosage: 400 mg/d PO in chronic-phase CML and GIST and 600 mg/d PO for CML in accelerated phase or blast crisis/800 mg/d PO (dermatofibrosarcoma protuberans)
Toxicities may include: Nausea and vomiting, edema and fluid retention, myalgias, diarrhea, myelosuppression, transaminitis
Use: Melanoma
Dosage: 3 mg/kg IV over 90 minutes every 3 weeks for a total of 4 doses
Toxicities may include: Fatigue, immune-mediated adverse reactions (diarrhea/colitis, pruritus, rash, hepatitis/elevated liver function tests, hypopituitarism, hypo-/hyperthyroidism, uveitis, pneumonitis, nephritis, pancreatitis, aseptic meningitis, neuromuscular disorders)
Use: Colorectal cancer, lung, ovarian, and cervical cancers
Dosage: 125 mg/m2 IV over 90 min once weekly for 4 weeks; then 2-week rest or 350 mg/m2 every 21 days or 180 mg/m2 every 2 weeks
Toxicities may include: Bone marrow depression, diarrhea, nausea and vomiting, anorexia, weight loss
Use: Breast cancer (relapse)
Dosage: 40 mg/m2 IV over 3 hours every 3 weeks
Toxicities may include: Myelosuppression, peripheral sensory neuropathy, fatigue/asthenia, myalgia/arthralgia, alopecia, nausea, vomiting, stomatitis/mucositis, diarrhea, musculoskeletal pain, abdominal pain, palmar-plantar erythrodysesthesia syndrome, hypersensitivity reaction
Use: Gastroenteropancreatic neuroendocrine tumors
Dosage: 120 mg every 4 weeks
Toxicities may include: Abdominal pain, cholelithasis, headache, hyperglycemia, hypertension, injection site reactions, musculoskeletal pain, vomiting
Warnings/Precautions include: Bradycardia, blood glucose alterations, gallstones
Use: HER2-positive metastatic breast cancer, or in combination with letrozole for postmenopausal women with hormone receptor–positive breast cancer for whom hormonal therapy is indicated
Dosage: 1,250 mg PO daily × 21 days in combination with capecitabine at 2,000 mg/m2/d PO (divided doses) on days 1–14 of a repeating 21-day cycle
Toxicities may include: Diarrhea, hand-foot syndrome, nausea, rash, vomiting, fatigue, left ventricular ejection fraction decrease, pneumonitis, QT prolongation
Use: Multiple myeloma (relapse)
Dosage: 10 mg/d PO
Toxicities may include: Birth defects, neutropenia and thrombocytopenia, thrombosis
Use: Locally recurrent, metastatic, progressive, radioactive iodine–refractory differentiated thyroid cancer
Dosage: 24 mg PO once a day
Toxicites may include: Hypertension, cardiac dysfunction, arterial thrombotic events, hepatotoxicity, proteinuria, renal failure, renal impairment, gastrointestinal perforation, QT prolongation, hypocalcemia, reversible posterior leukoencephalopathy syndrome, hemorrhage, changes in thyroid stimulating hormone, embryo-fetal toxicity, fatigue, diarrhea, arthralgia, appetite suppression, weight loss, nausea/vomiting, stomatitis, headache, palmar-plantar erythrodysesthesia
Use: Brain tumors, Hodgkin lymphoma, gastrointestinal carcinomas, non–small-cell lung cancer
Dosage: 130 mg/m2 PO every 6 weeks; adjust dose in combination chemotherapy
Toxicities may include: Delayed bone marrow depression, nausea and vomiting, reversible hepatotoxicity, pulmonary and renal damage, neurologic reactions, leukemia
Use: Hodgkin lymphoma, non-Hodgkin lymphoma, chronic myeloid leukemia, chronic lymphocytic leukemia, mycosis fungoides, bronchogenic carcinoma, lymphosarcoma, polycythemia vera, malignant effusions (intracavitary)
Dosage: 0.4 mg/kg ideal body weight given as single dose or in divided doses of 0.1–0.2 mg/kg/d
Toxicities may include: Bone marrow depression, nausea and vomiting, local phlebitis, severe skin necrosis if extravasated, gonadal dysfunction
Use: Multiple myeloma, breast and ovarian cancers, sarcoma, testicular cancer, and lung cancer
Dosage: Continuous therapy: 6 mg PO daily for 2–3 weeks, no therapy for 2–4 weeks, then maintenance with 2–4 mg PO daily. For pulse therapy: 10 mg/m2 PO daily for 4 days every 4–6 weeks
Toxicities may include: Bone marrow depression, anorexia, nausea and vomiting, gonadal testicular dysfunction, leukemia
Use: Acute lymphoblastic leukemia, chronic myeloid leukemia, acute myeloid leukemia
Dosage: 1.5–2.5 mg/kg/d PO (100–200 mg in average adult) until patient responds to treatment or toxic effects are seen; may increase dose to 5 mg/kg/d; adjust for maintenance dose; reduce dose by 50%-75% if given with allopurinol or if renal or hepatic insufficiency ensues
Toxicities may include: Bone marrow depression, nausea and vomiting, anorexia, diarrhea, cholestasis
Use: Breast, head and neck, gastrointestinal, and lung cancers, acute lymphoblastic leukemia, central nervous system leukemia (intrathecal), gestational trophoblastic tumors, non-Hodgkin lymphoma (advanced stage), Burkitt lymphoma, osteosarcoma, mycosis fungoides
Dosage: Numerous dosing schedules with combination therapy. Low dose: 2.5–5.0 mg PO daily; or 5–25 mg/m2 PO, IM, IV twice weekly; or 50 mg/m2 IV every 2–3 weeks; high dose: 1–12 g/m2 IV with leucovorin rescue every 1–3 weeks; intrathecal: 5–10 mg/m2 (up to 15 mg) every 3–7 days
Toxicities may include: Mucositis, gastrointestinal ulceration (may produce hemorrhage or perforation), bone marrow depression, pulmonary fibrosis (previously irradiated area), nerve root irritation and convulsion (intrathecal), liver cirrhosis and osteoporosis (chronic therapy), renal damage (high dose), diarrhea, skin erythema
Use: Gastric, colorectal, anal cancer, pancreatic adenocarcinomas, non–small-cell lung cancer, breast, uterine, cervical, and head and neck cancers
Dosage: 20 mg/m2 IV every 6–8 weeks as a single agent or 5–10 mg/m2 IV every 6 weeks in combination therapy
Toxicities may include: Bone marrow depression (cumulative), nausea and vomiting, anorexia, alopecia, stomatitis, fever, pulmonary fibrosis
Use: Acute myeloid leukemia, prostate, acute lymphoblastic leukemia, chronic myeloid leukemia, breast and ovarian cancers
Dosage: Remission induction: 12 mg/m2/d IV for 3 days, in combination with Ara-C
Toxicities may include: Bone marrow depression, cardiotoxicity, alopecia, stomatitis, nausea and vomiting, blue urine and sclera
Use: Chronic myeloid leukemia (CML)
Dosage: Newly diagnosed CML (chronic phase): 300 mg PO twice daily; resistant or intolerant CML(chronic phase or accelerated phase): 400 mg PO twice daily
Toxicities may include: Myelosuppression, hyperbilirubinemia, rash, pruritus, nausea, headache, fatigue, constipation, elevated lipase, QTc prolongation
Use: Unresectable or metastatic melanoma after ipilimumab or BRAF inhibitor, if BRAF V600–positive. Non–small-cell lung cancer with progression on or after a platinum-based chemotherapy
Dosage: 3 mg/kg every 2 weeks
Toxicities may include: Immune-mediated complications including: pneumonitis, colitis, hepatitis, nephritis, renal dysfunction, hyperthyroidism, hypothyroidism, embryo-fetal toxicity. Other toxicities may include: rash, fatigue, dyspnea, musculoskeletal pain, decreased appetite, cough, nausea, and constipation
Use: Chronic lymphocytic leukemia (CLL) refractory to fludarabine and alemtuzumab; and in combination with chlorambucil for CLL patients who would not tolerate fludarabine.
Dosage: Premedicate with acetaminophen PO, antihistamine PO or IV, and corticosteroids IV. For CLL refractory to fludarabine and alemtuzumab: 300 mg initial dose, followed 1 week later by 2,000 mg weekly for 7 doses, followed 4 weeks later by 2,000 mg every 4 weeks for 4 doses. For CLL in combination with chlorambucil: 300 mg on day 1, followed by 1,000 mg on day 8, then 1,000 mg on day 1 of a 28-day cycle for a minimum of 3 cycles, up to a maximum of 12 cycles.
Toxicities may include: Cytopenias, including neutropenia, infection, infusion reactions, fatigue, rash, tumor lysis syndrome, pneumonia, pyrexia, cough, diarrhea, dyspnea, nausea, bronchitis, upper respiratory tract infections
Use: Ovarian cancer
Dosage: 400 mg by mouth twice a day
Toxicities may include: Anemia, arthralgia/musculoskeletal pain/discomfort, cough, decreased appetite, diarrhea, dyspepsia, dysgeusia, fatigue/asthenia, headache, nausea, nasopharyngitis/pharyngitis/upper respiratory infection, and vomiting
Warnings/Precautions include: Embryo-fetal toxicity, pneumonitis, myelodysplastic syndrome/acute myeloid leukemia
Use: Colorectal, ovarian cancers
Dosage: 85 mg/m2 oxaliplatin and 200 mg/m2 leucovorin IV infusion over 120 min on day 1 followed by a 400 mg/m2 fluorouracil (5-FU) IV bolus, then 600 mg/m2 5-FU by IV infusion over 22 hours. On day 2, dose at 200 mg/m2 IV over 120 minutes IV, followed by 400 mg/m2 5-FU IV bolus, 600 mg/m2 5-FU IV infusion over 22 hours. Repeat every 2 weeks.
Toxicities may include: Bone marrow depression, diarrhea, nausea and vomiting, neuropathies exacerbated by cold exposure, pharyngolaryngeal dysesthesia, pulmonary toxicity
Use: Ovarian cancer (relapsed); non–small-cell lung cancer (in combination with cisplatin); Kaposi sarcoma; breast, head and neck, gastric, colon, esophagus, uterine, prostate, and bladder cancers; and melanomas
Dosage: 135–175 mg/m2 by IV infusion (ranging from 3–96 hours) every 3 weeks or 80 mg/m2 IV every week
Toxicities may include: Bone marrow depression, peripheral neuropathy, alopecia, mucositis, anaphylaxis, dyspnea, myalgias
Use: Estrogen receptor–positive, HER2-negative breast cancer, in combination with letrozole
Dosage: 125 mg PO daily with food on days 1–21 of a 28-day cycle
Toxicities may include: Neutropenia, infections, embryo-fetal toxicities, fatigue, anemia, upper respiratory tract infections, nausea, stomatitis, alopecia, diarrhea, thrombocytopenia, decreased appetite, vomiting, asthenia, peripheral neuropathy, epistaxis
Use:KRAS wild-type colorectal cancer
Dosage: 6 mg/kg IV over 60 minutes every 14 days
Toxicities may include: Skin rash, hypomagnesemia, paronychia, fatigue, infusion reactions, nausea/vomiting, diarrhea
Use: Renal cell carcinoma
Dosage: 800 mg PO once daily, without food
Toxicities may include: Diarrhea, hypertension, hair color change, nausea/vomiting, fatigue, anorexia
Use: Multiple myeloma in combination with bortezomib and dexamethasone
Dosage: 20 mg PO on days 1, 3, 5, 8, 10, and 12 of a 21-day cycle
Toxicities may include: Hemorrhage, hepatotoxicity, embryo-fetal toxicity, diarrhea, fatigue, nausea, peripheral edema, decreased appetite, pyrexia, and vomiting. Other laboratory and hematologic toxicities may occur.
Use: Acute lymphoblastic leukemia, chronic myeloid leukemia, acute myeloid leukemia
Dosage: 6,000 IU/m2 IM 3 times weekly for 9 doses or 100 IU/kg/d IV for 10 continuous days, starting on day 22 of treatment; usually given with vincristine and prednisone
Toxicities may include: Allergic reactions (fever, chills, skin rash, anaphylaxis), nausea and vomiting, anorexia, liver dysfunction, central nervous system depression, coagulopathy, hyperglycemia
Use: Melanoma
Dosage: 6 μg/kg/week SC for 8 doses followed by 3 μg/kg/week SC for up to 5 years
Toxicities may include: Fatigue, depression, anorexia, increased ALT/AST, myalgia, chills, nausea, headache, pyrexia, injection site reaction
Use: Metastatic melanoma
Dosage: 2 mg/kg intravenously over 30 minutes every 3 weeks
Toxicities may include: Immune-mediated reactions, including pneumonitis, colitis, hepatitis, hypophysitis, nephritis, and thyroid dysfunction. Other adverse effects include embryo-fetal toxicity, fatigue, cough nausea, pruritus, rash, decreased appetite, constipation, arthralgia, diarrhea.
Use: Mesothelioma, non–small-cell lung cancer
Dosage: 500 mg/m2 IV over 10 minutes every 21 days. Premedication needed with corticosteroid and vitamin supplementation
Toxicities may include: Bone marrow depression, stomatitis/pharyngitis, rash/skin desquamation, diarrhea
Use: Hairy-cell leukemia, acute lymphoblastic leukemia, chronic lymphocytic leukemia, lymphoblastic lymphoma, mycosis fungoides
Dosage: 4 mg/m2 IV over 30 minutes every other week or for 3 consecutive weeks; give vigorous hydration before and after chemotherapy
Toxicities may include: Nephrotoxicity, central nervous system depression, bone marrow depression, nausea and vomiting, conjunctivitis
Use: Relapsed and refractory T-cell lymphoma
Dosage: 30 mg/m2 administered as an IV push over 3 to 5 minutes once weekly in 7-week cycles. Supplement with vitamin B-12, 1 mg IM every 8–10 weeks, and folic acid at 1–1.25 mg PO daily
Toxicities may include: Mucositis, thrombocytopenia, nausea, fatigue, febrile neutropenia
Use: Hodgkin lymphoma (HL), non-Hodgkin lymphoma, brain tumors, lung cancer
Dosage: Single agent: 4–6 mg/kg/d PO until maximum response; HL (mechlorethamine,
Oncovin [vincristine], procarbazine, and prednisone [MOPP]): 100 mg/m2/d PO for 14 days
Toxicities may include: Bone marrow depression, nausea and vomiting, lethargy, depression, paresthesias, headache, flu-like symptoms
Use: Gastric cancer, non–small-cell lung cancer (NSCLC), colorectal cancer
Dosage: Gastric cancer: 8 mg/kg IV every 2 weeks, alone or in combination with paclitaxel; NSCLC: 10 mg/kg IV on day 1 of a 21-day cycle, prior to docetaxel; colorectal cancer: 8 mg/kg IV every 2 weeks, prior to FOLFIRI
Toxicities may include: asthenia, diarrhea, epistaxis, fatigue, hypertension, neutropenia, stomatitis/mucositis, gastric perforations, hemorrhage, hypertension, impaired wound healing, proteinuria, thyroid dysfunction
Use: CD20-positive B-cell non-Hodgkin lymphoma, chronic lymphocytic leukemia
Dosage: 375 mg/m2 IV infusion (50–100 mg/h) once weekly in combination with fludarabine and cyclophosphamide; rituximab 375 mg/m2 (first cycle) and 500 mg/m2 in cycles 2–6
Toxicities may include: Infusion reactions, asthenia, headache, skin rash/pruritus, leukopenia/infection, nausea, tumor lysis syndrome, hepatitis B reactivation, progressive multifocal leukoencephalopathy
Use: Cutaneous T-cell lymphoma refractory to 1 prior systemic therapy
Dosage: 14 mg/m2 IV over 4 hours on days 1, 8, and 15 of a 28-day cycle
Toxicities may include: Myelosuppression, QT prolongation (make sure magnesium and potassium are normal prior to administration), nausea, fatigue
Use: Myelofibrosis, polycythemia vera in patients who failed to respond to, or were intolerant of, treatment with hydroxyurea
Dosage: Starting dose for patients with myelofibrosis: 5–20 mg PO twice daily; polycythemia vera: 10 mg PO twice daily
Toxicities may include: Thrombocytopenia, anemia, bruising, dizziness, headache, infections, nonmelanoma skin cancers
Use: Asymptomatic or minimally symptomatic metastatic castrate-resistant (hormone-refractory) prostate cancer
Dosage: Administer 3 doses at approximately 2-week intervals. Premedicate patients with acetaminophen and antihistamine. Infuse sipuleucel-T IV over a period of 60 minutes. Each dose contains a minimum of 50 million autologous CD54+ cells activated with prostatic acid phosphatase granulocyte-macrophage colony stimulating factor suspended in 250 mL of lactated Ringer’s injection.
Toxicities may include: Chills, fever, back pain, nausea, joint ache, headache
Use: Renal cell cancer, hepatocellular carcinoma
Dosage: 400 mg PO twice a day
Toxicities may include: Diarrhea, nausea, stomatitis, asthenia, cardiac ischemia, hand-foot syndrome, hypertension, bleeding, anorexia
Use: Pancreatic islet-cell, carcinoid, colon, hepatoma, non–small-cell lung cancer, Hodgkin lymphoma
Dosage: daily: 500 mg/m2 IV for 5 days every 6 weeks until maximum benefit or toxicity; weekly: 1,000 mg/m2 IV weekly for first 2 weeks, then escalate dose to response or toxicity, not to exceed a single dose of 1,500 mg/m²
Toxicities may include: Renal damage, nausea and vomiting, diarrhea, altered glucose metabolism, liver dysfunction
Use: Renal cell cancer, gastrointestinal stromal tumor, pancreatic neuroendocrine tumors (PNETs)
Dosage: 50 mg/d PO for 4 weeks, then 2-week rest period; PNETs: 37.5 mg PO daily continuously
Toxicities may include: Diarrhea, nausea, stomatitis, asthenia, skin discoloration, hand-foot syndrome, hypertension, bleeding, anorexia, hepatotoxicity, cardiac toxicity, thyroid dysfunction
Use: Glioblastoma, anaplastic astrocytoma (relapsed), renal cell carcinoma, melanoma
Dosage: 150–200 mg/m2/d PO for 5 days every 28 days; 75 mg/m2 PO/d concomitant with radiotherapy
Toxicities may include: Bone marrow depression, nausea and vomiting
Use: Renal cell carcinoma
Dosage: 25 mg IV weekly over 30–60 minutes
Toxicities may include: Rash, asthenia, mucositis, edema, dyslipidemia, hyperglycemia, elevated serum creatinine. Rarely, interstitial lung disease
Use: Relapsed acute lymphoblastic leukemia (ALL) in children, small-cell lung cancer
Dosage: ALL: 100 mg/m2 once or twice weekly or 20–60 mg/m2/d for 5 days in combination with Ara-C; lung: 80–90 mg/m2/d for 5 days as a single agent
Toxicities may include: Bone marrow depression, nausea and vomiting, alopecia, hypotension with rapid infusion, increased levels of liver enzymes, acute myeloid leukemia (late effect)
Use: Multiple myeloma
Dosage: 200 mg/d PO
Toxicities may include: Birth defects, thrombotic events, somnolence, peripheral neuropathy, neutropenia
Use: acute myeloid leukemia, acute lymphoblastic leukemia, chronic myeloid leukemia, advanced colorectal cancer, multiple myeloma
Dosage: 2 mg/kg/d PO until patient responds to treatment or toxic effects are seen; may cautiously increase to 3 mg/kg/d
Toxicities may include: Bone marrow depression, liver damage, stomatitis
Use: Ovarian, breast, and superficial bladder cancers, Hodgkin lymphoma, chronic myeloid leukemia, chronic lymphocytic leukemia, bronchogenic carcinoma, malignant effusions (intracavitary), bone marrow transplant for refractory leukemia, lymphomas
Dosage: IV: 0.3–0.4 mg/kg by rapid IV infusion; intravesical: 60 mg/60 mL sterile water instilled and retained in bladder for 2 hours, repeated weekly for 4 weeks; intracavitary: 0.6–0.8 mg/kg
Toxicities may include: Bone marrow depression, nausea and vomiting, mucositis, skin rashes
Use: Cervical cancer, ovarian cancer (relapsed), small-cell lung cancer (relapsed), myelodysplastic syndrome, chronic myelomonocytic leukemia
Dosage: 1.5 mg/m2 IV over 30 min for 5 consecutive days at 21-day intervals or 2.3 mg/m2/d PO for 5 consecutive days every 21 days
Toxicities may include: Bone marrow depression, fever, flu-like symptoms, nausea and vomiting
Use: CD20+ low-grade follicular or transformed non-Hodgkin lymphoma (relapse)
Dosage: dosimetric step, on day 1: tositumomab 450 mg IV over 60 min, I-131 tositumomab (5 mCi and 35 mg tositumomab) IV over 20 minutes; therapeutic step on days 7–14: tositumomab 450 mg IV over 60 min; I-131 tositumomab calculated
Toxicities may include: Myelosuppression, hypothyroidism, second malignancies
Use: Patients with unresectable or metastatic melanoma with BRAF V600E mutations or BRAF V600K mutations who have not received prior BRAF-inhibitor therapy
Dosage: 2 mg PO once a day on an empty stomach
Toxicities may include: Retinal pigment epithelial detachment, retinal vein occlusion, interstitial lung disease, skin infections or rash, embryo-fetal toxicity, diarrhea, lymphedema
Use: HER2-overexpressing breast cancer, HER2-overexpressing gastric cancer
Dosage: 4 mg/kg IV over 90 min, loading dose, and 2 mg/kg IV over 30 minutes every 7 days, as maintenance; or 8 mg/kg loading dose and 6 mg/kg every 21 days as maintenance
Toxicities may include: Cardiac failure, infusion reaction, diarrhea
Use: Bladder
Dosage: 800 mg intravesically once a week for 6 weeks
Toxicities may include: Local bladder symptoms
Use: Medullary thyroid cancer
Dosage: 300 mg PO daily
Toxicities may include: Prolonged QT interval, torsades de pointes, sudden death, diarrhea, rash, acne, nausea, hypertension, headache, fatigue, decreased appetite and abdominal pain, decreased calcium, increased ALT levels, decreased glucose levels
Use: Melanoma with a BRAF V600E mutation
Dosage: 960 mg PO twice daily, administered approximately 12 hours apart, with or without a meal
Toxicities may include: Arthralgia, rash, alopecia, fatigue, photosensitivity reaction, nausea, squamous cell carcinomas of the skin and keratoacanthomas, hypersensitivity, Stevens-Johnson syndrome, toxic epidermal necrolysis, uveitis, QT prolongation, liver enzyme laboratory abnormalities
Use: Hodgkin lymphoma, non-Hodgkin lymphoma, gestational trophoblastic tumors, testicular and breast cancers, mycosis fungoides, Kaposi sarcoma, histiocytosis X, bladder and renal cancers, non–small-cell lung cancer, chronic myeloid leukemia (blast crisis)
Dosage: 4–12 mg/m2 IV as a single agent every 1–2 weeks; titrate dose to myelosuppression; adjust for hepatic insufficiency
Toxicities may include: Bone marrow depression, nausea and vomiting, ileus, alopecia, stomatitis, myalgias, vesication
Use: Acute lymphoblastic leukemia, Hodgkin lymphoma, non-Hodgkin lymphoma, rhabdomyosarcoma, neuroblastoma, Wilms tumor, multiple myeloma, sarcomas, breast cancer
Dosage: 0.4–1.4 mg/m2 IV weekly; maximum total dose, 2 mg/week; reduce dose for hepatic insufficiency
Toxicities may include: Peripheral neuropathy, ileus, abdominal pain, syndrome of inappropriate antidiuretic hormone secretion, bone marrow depression (mild)
Use: Non–small-cell lung cancer, breast, ovarian, head and neck cancers, Hodgkin lymphoma
Dosage: 30 mg/m2 IV over 10 minutes; repeat weekly
Toxicities may include: Peripheral neuropathy, bone marrow depression, nausea, vomiting, hepatic dysfunction
Efficacy and Safety of Zolbetuximab in Gastric Cancer
Zolbetuximab’s targeted action, combined with manageable adverse effects, positions it as a promising therapy for advanced gastric cancer.
These data support less restrictive clinical trial eligibility criteria for those with metastatic NSCLC. This is especially true regarding both targeted therapy and immunotherapy treatment regimens.