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docetaxel (Taxotere, Docefrez)

Tradename: Taxotere. Indications: - locally advanced or metastatic breast cancer with progression or relapse after anthracycline therapy - ovarian cancer - gastric cancer [3] - small cell carcinoma - non small cell carcinoma - Ewing sarcoma - osteosarcoma - esophageal cancer - bladder cancer - androgen-independent prostate cancer [3] Contraindications: Caution: - severe hypersensitivity in 25% of patients not receiving premedication docetaxel administration Dosage: - premedication with dexamethasone 16 mg PO QD for 3 days starting 1 day prior to administration of docetaxel - 60-100 mg/m2 IV over 1 hr q3weeks [7] - 75 mg/m2 most common dosage Injection: - 10 mg/mL (2mL, 8mL, 16mL vials) - 20 mg/mL (1mL, 4mL vials) - 40 mg/mL (0.5 mL, 2 mL) (contains ethanol) [4] Pharmacokinetics: 1) extensive extravascular distribution 2) protein binding 94%, largely albumin, alpha-1 acid glycoprotein & lipoproteins 3) metabolism by cyt P450 3A 4) triphasic elimination: 1/2lives 4 min, 36 min & 11 hours Adverse effects: 1) common (> 10%) - fever, alopecia (nearly all patients), nausea/vomiting, diarrhea, stomatitis, neutropenia (dose-limiting), leukopenia, thrombocytopenia, anemia, myalgia 2) not common (1-10%) - fluid retention syndrome: - pleural effusion, edema, ascites - incidence & severity increase markedly at cumulative doses of > 400 mg/m2 - dyspnea at rest - cardiac tamponade (due to ascites) 3) uncommon (< 1%) - hypersensitivity reactions 4) other - symptoms of alcohol intoxication (contains ethanol) [4] - hand & foot syndrome [5] - cumulative dose may be associated with persisitent peripheral neuropathy in breast cancer survivors [6] Drug interactions: - possibly increased toxicity with: a) ketoconazole b) erythromycin c) terfenadine d) astemizole e) cisapride f) cyclosporine

General

antimitotic agent; mitotic inhibitor (antineoplastic agent) taxane

Properties

MISC-INFO: elimination route LIVER 1/2life 11 HOURS pregnancy-category D

Database Correlations

PUBCHEM correlations

References

  1. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  2. Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 529
  3. Deprecated Reference
  4. FDA Safety Announcement: June 20, 2014 FDA Drug Safety Communication: FDA warns that cancer drug docetaxel may cause symptoms of alcohol intoxication after treatment. http://www.fda.gov/Drugs/DrugSafety/ucm401752.htm
  5. Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015
  6. Davenport L Neuropathy After Breast Cancer Chemo Can Last for Years. Medscape - Sep 01, 2017. http://www.medscape.com/viewarticle/885106 - Bandos H, Melnikow J, Rivera DR et al Long-term Peripheral Neuropathy in Breast Cancer Patients Treated With Adjuvant Chemotherapy: NRG Oncology/NSABP B-30. JNCI: Vol 110, Issue 2, 1 Feb 2018; Online Aug 24, 2017 PMID: 28954297 https://academic.oup.com/jnci/article-abstract/110/2/djx162/4093779/Long-term-Peripheral-Neuropathy-in-Breast-Cancer
  7. Medscape: docetaxel https://reference.medscape.com/drug/taxotere-docetaxel-342192

Component-of

doxorubicin (Adriamycin)/docetaxel (Taxotere)