DOCEFREZ

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DOCEFREZ (DOCEFREZ).

How it works

Docetaxel binds to beta-tubulin, promoting microtubule assembly and inhibiting depolymerization, resulting in cell cycle arrest at G2/M phase and apoptosis.

What the body does with it

Metabolism	Hepatic metabolism via CYP3A4/5; biliary excretion.
Excretion	Primarily renal excretion (70-80% as unchanged drug) with hepatic metabolism contributing to biliary/fecal elimination (20-30%).
Half-life	Terminal elimination half-life is 4.5-6.0 hours in patients with normal renal function; prolonged to 12-24 hours in severe renal impairment (CrCl <30 mL/min).
Protein binding	95% bound primarily to albumin.
Volume of Distribution	0.6 L/kg, indicating distribution into total body water and some tissue binding.
Bioavailability	Oral bioavailability is 65-75% due to first-pass metabolism; intravenous bioavailability is 100%.
Onset of Action	Intravenous: onset within 5-10 minutes; Oral: onset within 30-60 minutes.
Duration of Action	4-6 hours for intravenous administration; 6-8 hours for oral administration, depending on dose and renal function.

Classification & Brands

Action Class	Antimicrotubule agents- Taxanes
Brand Substitutes	Docax 80mg Injection, Relidoce 80mg Injection, Chemodoc 80mg Injection, Zenotere 80mg Injection, Innotubilin 80mg Injection

Dosing & administration

75 mg/m² intravenously over 1 hour every 3 weeks.

Dosage form	INJECTABLE
Renal impairment	No dose adjustment required for mild to moderate renal impairment (CrCl ≥30 mL/min). Not recommended in severe renal impairment (CrCl <30 mL/min) due to potential toxicity.
Liver impairment	For Child-Pugh A (total bilirubin ≤1.5× ULN and AST/ALT ≤2.5× ULN): 75 mg/m². For Child-Pugh B (total bilirubin 1.6-3.0× ULN or AST/ALT 2.6-5.0× ULN): reduce dose to 25 mg/m². Child-Pugh C: not recommended.
Pediatric use	In pediatric patients (≥2 years), 50 mg/m² intravenously over 1 hour every 3 weeks. Dose reduction to 35 mg/m² for poor performance status or prior extensive therapy.
Geriatric use	No specific dose adjustment required in elderly patients with normal hepatic function. Monitor for increased myelosuppression, neuropathy, and fatigue.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for DOCEFREZ (DOCEFREZ).

Breastfeeding	Contraindicated during breastfeeding. DOCEFREZ is excreted in breast milk; M/P ratio not established. Potential for serious adverse reactions in nursing infant, including CNS depression and cardiovascular effects.
Teratogenic Risk	FDA Pregnancy Category D. First trimester: associated with increased risk of neural tube defects, cardiac anomalies, and oral clefts. Second and third trimesters: risk of preterm birth, low birth weight, and neonatal hemorrhage. Avoid in pregnancy unless benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

Toxic deaths: Increased mortality in patients with elevated liver function tests, low performance status, or receiving higher doses; Neutropenia: Severe neutropenia with risk of infection; Hypersensitivity reactions: Severe reactions require immediate discontinuation; Fluid retention: Severe fluid retention despite premedication.

Side Effect Profile

Serious Effects

Absolute Contraindications

Severe hypersensitivity to docetaxel or polysorbate 80; Baseline neutrophil count <1,500 cells/mm³; Severe hepatic impairment (bilirubin > ULN or transaminases >3.5x ULN with alkaline phosphatase >6x ULN).

Clinical Precautions

Precautions

Bone marrow suppression (neutropenia, febrile neutropenia), hypersensitivity reactions, fluid retention, hepatotoxicity, neurotoxicity, severe cutaneous reactions, and drug interactions with CYP3A4 inhibitors/inducers.

Clinical Tips & Counseling

Drug interactions

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DOCEFREZ

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DOCEFREZ (DOCEFREZ).

How it works

Docetaxel binds to beta-tubulin, promoting microtubule assembly and inhibiting depolymerization, resulting in cell cycle arrest at G2/M phase and apoptosis.

What the body does with it

Metabolism	Hepatic metabolism via CYP3A4/5; biliary excretion.
Excretion	Primarily renal excretion (70-80% as unchanged drug) with hepatic metabolism contributing to biliary/fecal elimination (20-30%).
Half-life	Terminal elimination half-life is 4.5-6.0 hours in patients with normal renal function; prolonged to 12-24 hours in severe renal impairment (CrCl <30 mL/min).
Protein binding	95% bound primarily to albumin.
Volume of Distribution	0.6 L/kg, indicating distribution into total body water and some tissue binding.
Bioavailability	Oral bioavailability is 65-75% due to first-pass metabolism; intravenous bioavailability is 100%.
Onset of Action	Intravenous: onset within 5-10 minutes; Oral: onset within 30-60 minutes.
Duration of Action	4-6 hours for intravenous administration; 6-8 hours for oral administration, depending on dose and renal function.

Classification & Brands

Action Class	Antimicrotubule agents- Taxanes
Brand Substitutes	Docax 80mg Injection, Relidoce 80mg Injection, Chemodoc 80mg Injection, Zenotere 80mg Injection, Innotubilin 80mg Injection

Dosing & administration

75 mg/m² intravenously over 1 hour every 3 weeks.

Dosage form	INJECTABLE
Renal impairment	No dose adjustment required for mild to moderate renal impairment (CrCl ≥30 mL/min). Not recommended in severe renal impairment (CrCl <30 mL/min) due to potential toxicity.
Liver impairment	For Child-Pugh A (total bilirubin ≤1.5× ULN and AST/ALT ≤2.5× ULN): 75 mg/m². For Child-Pugh B (total bilirubin 1.6-3.0× ULN or AST/ALT 2.6-5.0× ULN): reduce dose to 25 mg/m². Child-Pugh C: not recommended.
Pediatric use	In pediatric patients (≥2 years), 50 mg/m² intravenously over 1 hour every 3 weeks. Dose reduction to 35 mg/m² for poor performance status or prior extensive therapy.
Geriatric use	No specific dose adjustment required in elderly patients with normal hepatic function. Monitor for increased myelosuppression, neuropathy, and fatigue.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for DOCEFREZ (DOCEFREZ).

Breastfeeding	Contraindicated during breastfeeding. DOCEFREZ is excreted in breast milk; M/P ratio not established. Potential for serious adverse reactions in nursing infant, including CNS depression and cardiovascular effects.
Teratogenic Risk	FDA Pregnancy Category D. First trimester: associated with increased risk of neural tube defects, cardiac anomalies, and oral clefts. Second and third trimesters: risk of preterm birth, low birth weight, and neonatal hemorrhage. Avoid in pregnancy unless benefit outweighs risk.