DOCEtaxel (doe-se-tax-el) Docefrez, Taxotere

 Indications

Breast cancer (locally advanced/metastatic breast cancer

or with doxorubicin and cyclophosphamide as adjuvant

treatment of node-positive disease). Non–smallcell

lung cancer (locally advanced/metastatic) after

failure on platinum regimen or with platinum as initial

therapy). Advanced metastatic hormone-refractory

prostate cancer (with prednisone). Squamous cell carcinoma

of the head and neck (locally advanced) with

cisplatin and fluorouracil. Gastric adenocarcinoma (locally

advanced) with cisplatin and fluorouracil.

Action

Interferes with normal cellular microtubule function

required for interphase and mitosis. Therapeutic

Effects: Death of rapidly replicating cells, particularly

malignant ones.

Pharmacokinetics

Absorption: IV administration results in complete

bioavailability.

Distribution: Unknown.

Metabolism and Excretion: Extensively metabolized

by the liver; metabolites undergo fecal elimination.

Half-life: 11.1 hr.

TIME/ACTION PROFILE (effect on blood

counts)

ROUTE ONSET PEAK DURATION

IV rapid 5–9 days 7 days

Contraindications/Precautions

Contraindicated in: Hypersensitivity; Hypersensitivity

to polysorbate 80; Known alcohol intolerance;

Neutrophil count 1500/mm3; Liver impairment (serum

bilirubin upper limit of normal, ALT and/or AST

1.5 times upper limit of normal, with alkaline phosphatase

2.5 times upper limit of normal); OB, Lactation:

Pregnancy or lactation.

Use Cautiously in: OB: Patients with child-bearing

potential; Pedi: Efficacy not established.

Adverse Reactions/Side Effects

CNS: fatigue, weakness, alcohol intoxication. EENT:

cystoid macular edema. Resp: ACUTE RESPIRATORY DISTRESS

SYNDROME, INTERSTITIAL LUNG DISEASE, PULMONARY

FIBROSIS, bronchospasm, dyspnea. CV: ASCITES, CARDIAC

TAMPONADE, PERICARDIAL EFFUSION, PULMONARY

EDEMA, peripheral edema. GI: diarrhea, nausea, stomatitis,

vomiting. Derm: alopecia, edema, rash, dermatitis,

desquamation, erythema, nail disorders. Hemat:

anemia, leukopenia, thrombocytopenia,

leukemia. Local: injection site reactions. MS: myalgia,

arthralgia. Neuro: neurosensory deficits, peripheral

neuropathy. Misc: hypersensitivity reactions, including

ANAPHYLAXIS. 

Interactions

Drug-Drug:qbone marrow depression may occur

with other antineoplastics or radiation therapy.

Strong inhibitors of CYP3A4, including atazanavir,

clarithromycin, indinavir, itraconazole, ketoconazole,

nefazodone, nelfinavir, ritonavir, saquinavir,

or voriconazoleqlevels and the risk of toxicity;

avoid concomitant use (if need to use,pdocetaxel dose

by 50%).

Route/Dosage

IV (Adults): Breast cancer—60–100 mg/m2 every 3

wk; Breast cancer adjuvant therapy—75 mg/m2

every 3 wk for 6 cycles (with doxorubicin and cyclophosphamide);

Non–small-cell lung cancer—75

mg/m2 every 3 wk (alone or with platinum); Prostate

cancer—75 mg/m2 every 3 wk (with oral prednisone);

Squamous cell head and neck cancer—75

mg/m2 every 3 wk for 3–4 cycles (with cisplatin and

fluorouracil); Gastric adenocarcinoma—75 mg/m2

every 3 wk (with cisplatin and fluorouracil).

Availability (generic available)

Injection concentrate: 10 mg/mL (dose of 100 mg/

m2 contains 0.15 g/m2 of ethanol), 20 mg/mL (dose of

100 mg/m2 contains 1.975 g/m2 of ethanol), 40 mg/mL

(dose of 100 mg/m2 contains 0.15 g/m2 of ethanol).

Lyophilized powder for injection: 20 mg/vial, 80

mg/vial.