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Chemotherapeutic Agents and Their Uses, Dosages, and Toxicities

Chemotherapeutic Agents and Their Uses, Dosages, and Toxicities


Abiraterone acetate

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

Albumin-bound (nab) paclitaxel

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

Brentuximab vedotin

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)

Cytarabine (Ara-C)

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

DaunoXome (liposomal daunorubicin)

Use: Kaposi sarcoma, acute lymphoblastic leukemia, acute myeloid leukemia

Dosage: Liposomal preparation: 40 mg/m2 IV every 2 weeks

DepoCyt (liposomal cytarabine)

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

Doxil (liposomal doxorubicin)

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


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