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Chemotherapeutic Agents and Their Uses, Dosages, and Toxicities

Chemotherapeutic Agents and Their Uses, Dosages, and Toxicities

Selected chemotherapeutic agents and their uses, dosages, and toxicities.


Abiraterone acetate

Use: Metastatic castration-resistant prostate cancer

Dosage: 1,000 mg PO qd (empty stomach) in combination with prednisone 5 mg orally twice daily

Toxicities: Joint swelling or discomfort, hypokalemia, edema, muscle discomfort, hot flushes, diarrhea, urinary tract infection, cough, hypertension, arrhythmia, urinary frequency, nocturia, dyspepsia, upper respiratory tract infection, Increases in liver enzymes, adrenocortical insufficiency

Albumin-bound (nab) paclitaxel

Use: Breast cancer (relapse)

Dosage: 260 mg/m2 IV over 30 min every 3 wk

Toxicities: Bone marrow depression, sensory neuropathy, arthralgia/myalgia, asthenia, abnormal ECG, alopecia


Use: Chemotherapy-refractory B-cell chronic lymphocytic leukemia (CLL)

Dosage: 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 min, 3 times per wk on alternate days for up to 12 wk

Toxicities: Pancytopenia, infusion reaction, opportunistic infections, skin rash, nausea/vomiting


Use: Ovarian, lung, breast, and cervical cancers, non-Hodgkin lymphoma (NHL)

Dosage: 4–12 mg/kg/d or 260 mg/m2, PO divided in 3–4 doses for 14–21 d of a 28-d regimen

Toxicities: Nausea and vomiting, bone marrow depression, paresthesias, CNS toxicity


Use: Acute lymphoblastic leukemia (ALL), chronic myelogenous leukemia (CML), acute myelogenous leukemia (AML)

Dosage: 6,000 IU/m2 IM 3 times weekly for 9 doses or 100 IU/kg/d IV for 10 continuous days, starting on D 22 of treatment; usually given with vincristine and prednisone

Toxicities: Allergic reactions (fever, chills, skin rash, anaphylaxis), nausea and vomiting, anorexia, liver dysfunction, CNS depression, coagulopathy, hyperglycemia


Use: CLL, B-cell NHL (relapse)

Dosage: IV: 100 mg/m2 on D 1 and D 2 of a 28-d cycle, up to 6 cycles

Toxicities: Bone marrow depression, fever, nausea, and vomiting


Use: Breast cancer, colorectal cancer, non–small-cell lung cancer (NSCLC), renal cell carcinoma, glioblastoma (relapse)

Dosage: 5 mg/kg/wk IV over 60–90 min every 14–21 d

Toxicities: Asthenia, headache, epistaxis, proteinuria, GI perforations/wound-healing complications, hypertension/hypertensive crisis; hemorrhage, thromboembolic event, ovarian failure, osteonecrosis of the jaw


Use: Testicular cancer, Hodgkin lymphoma (HL), reticulum cell sarcoma, 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: Pneumonitis and pulmonary fibrosis, fever and allergic reactions, anaphylaxis, hyperpigmentation, Raynaud’s phenomenon, alopecia


Use: Multiple myeloma

Dosage: 1.3 mg/m2 on D 1, 4, 8, and 11 every 3 wk

Toxicities: 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 2 prior multiagent chemotherapy regimens in patients who are not ASCT candidates; The treatment of patients with systemic anaplastic large-cell lymphoma after failure of at least 1 prior multiagent chemotherapy regimen.

Dosage: 1.8 mg/kg IV infusion over 30 minutes every 3 weeks (maximum 16 cycles)

Toxicities: Neutropenia, peripheral sensory neuropathy, abdominal pain, fatigue, nausea, anemia, upper respiratory tract infection, diarrhea, pyrexia, rash, thrombocytopenia, cough, vomiting


Use: CML, bone marrow transplantation (BMT) 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 < 15,000/µL; resume therapy when WBC count > 50,000/µL

Toxicities: 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 10 mg PO daily throughout cabazitaxel treatment. Premedicate 30 minutes before each dose with antihistamine, corticosteroid, and H2 antagonist.

Toxicities: Febrile neutropenia (primary G-CSF prophylaxis should be considered in high-risk patients), nausea, vomiting, diarrhea, renal failure, hypersensitivity reactions


Use: Breast cancer (relapsed), colorectal cancer, and other GI malignancies

Dosage: 1,250 mg/m2 bid PO with food (2 wk on drug, 1 wk of rest)

Toxicities: 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, NHL


Single agent: 360 mg/m2 IV every 4 wk

Combination: 300 mg/m2 IV every 4 wk

Calvert formula: Total dose (mg) = Target area under the curve (AUC) × (glomerular filtration rate [GFR] + 25)

Toxicities: Bone marrow depression, nausea and vomiting, peripheral neuropathy, ototoxicity

Total carboplatin dose calculation based on isotope dilution mass spectrometry (IDMS)-measured serum creatinine 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, HL, NHL, melanoma, BMT for refractory solid tumors and lymphomas

Dosage: 150–200 mg/m2 IV every 6–8 wk

Toxicities: Delayed bone marrow depression, nausea and vomiting, reversible hepatotoxicity, local phlebitis, pulmonary and renal damage (high dose)


Use: KRAS wild type colorectal cancer, head and neck cancer

Dosage: 400 mg/m2 IV over 120 min, loading dose, and 250 mg/m2 IV over 60 min every 7 d, as maintenance

Toxicities: Skin rash, infusion reaction, asthenia, diarrhea, nausea, hypomagnesemia


Use: CLL, HL, NHL, ovarian cancer, choriocarcinoma, lymphosarcoma

Dosage: 0.1–0.2 mg/kg PO daily for 3–6 wk as required (usually 4–10 mg/d) or intermittent 0.4 mg/kg every 3–4 wk; increase by 0.1 mg/kg until control of disease or toxicity

Toxicities: 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, NHL

Dosage: 50 mg/m2 IV or more every 3 wk; or 20 mg/m2 IV daily for 4–5 d every 3–4 wk; give vigorous hydration before and after chemotherapy

Toxicities: Renal damage, nausea and vomiting, electrolyte disturbance, peripheral neuropathy, bone marrow depression, ototoxicity, radiosensitizer


Use: Hairy-cell leukemia, NHL, mycosis fungoides, AML, CML, CLL

Dosage: 0.09 mg/kg/d (4 mg/m2/d) by continuous IV infusion for 7 consecutive days

Toxicities: Bone marrow depression, febrile episodes, rash, infections, septicemia


Use: NSCLC anaplastic lymphoma kinase (ALK)-mutation positive

Dosage: 250 mg orally twice daily

Toxicities: Vision disorder, nausea, diarrhea, vomiting, edema, constipation, increased ALT, neutropenia, pneumonitis


Use: AML, ALL, CLL, HL, and NHL, 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 d to start, followed by 10–15 mg/kg IV every 7–10 d; or 3–5 mg/kg IV twice weekly; or 1–5 mg/kg/d PO

Toxicities: Bone marrow depression, hemorrhagic cystitis, immunosuppression, alopecia, stomatitis, syndrome of inappropriate antidiuretic hormone secretion (SIADH)

Cytarabine (Ara-C)

Use: AML, ALL, CML, NHL, CNS leukemia (intrathecal)

Dosage: AML induction: 100 mg/m2/d by continuous IV infusion on D 1–7; or 100 mg/m2 IV every 12 h on D 1–7; Relapsed ALL: 3 g/m2 IV over 1–3 h every 12 h for 4 doses

Toxicities: Bone marrow depression, nausea and vomiting, diarrhea, arachnoiditis (intrathecal), stomatitis, hepatic dysfunction, fever, conjunctivitis, confusion, somnolence, cerebellar toxicity


Use: Malignant melanoma, HL, soft-tissue sarcomas, neuroblastoma


Melanoma: 2–4.5 mg/kg/d IV for 10 d every 4 wk; or 250 mg/m2/d IV for 5 d every 3 wk

HL: 375 mg/m2 IV on D 1, repeated every 15 d (single agent); 150 mg/m2/d IV for 5 d every 4 wk (combination therapy)

Toxicities: 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 d every 3 wk (usual adult dose, 0.5 mg) or 2 mg/m2 IV as a single dose every 3–4 wk

Toxicities: Stomatitis, bone marrow depression, anorexia, nausea and vomiting, diarrhea, alopecia, skin changes, anaphylactoid reaction


Use: CML, Ph+ ALL

Dosage: 140 mg/d (divided doses; 70 mg bid) or 100 mg/d PO (chronic phase CML)

Toxicities: Fluid-retention events (eg, pleural effusion); GI events: diarrhea, nausea, abdominal pain, vomiting; bleeding events; hematologic toxicities: neutropenia, thrombocytopenia, anemia



Dosage: Remission induction: 30–45 mg/m2/d IV for 3 d in combination therapy; total cumulative dose, 550 mg/m²

Toxicities: 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, ALL, AML

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

DepoCyt (liposomal cytarabine)

Use: CNS leukemia/lymphoma

Dosage: Intrathecal: DepoCyt, 50 mg over 1–5 min every 14 d, with dexamethasone, 4 mg PO bid × 5 d


Use: Breast, NSCLC, prostate, ovarian, pancreatic, head and neck, esophagus, stomach, cervical, Kaposi sarcoma, uterine, and bladder cancers

Dosage: 60–100 mg/m2 IV over 1 h every 21 d or up to 42 mg/m2 IV every wk

Toxicities: 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 wk 20 mg/m2 IV every 3 wk

Toxicities: Bone marrow depression, hand-foot syndrome, infusional reactions


Use: ALL, AML, breast, ovarian, bladder cancers, HL, NHL, small-cell lung cancer (SCLC), gastric cancer, sarcoma, Wilms’ tumor, neuroblastoma, thyroid cancer, soft-tissue and bone sarcomas

Dosage: 60–90 mg/m2 single IV injection every 21 d, 20–30 mg/m2/d IV for 3 d every 3–4 wk, or 20 mg/m2 IV weekly; total cumulative dose of 550 mg/m2; reduce dose for liver dysfunction

Toxicities: 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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