Cabazitaxel

Microtubule inhibitors
Microtubule inhibitors
High alert
An error with this medicine can cause serious harm: double checks and protocols are used.

Taxane that stabilises microtubules and escapes the P-glycoprotein pump. For castration-resistant prostate cancer after docetaxel; neutropenia can be fatal.

Updated Nov 1, 2026

Quick facts

Group: Microtubule inhibitors
Target: β-tubulin (taxane site, inside the microtubule)
Key effects: Diarrhoea · Tiredness · Taste changes
Monitor: Blood count often · Fluid balance · Liver tests
ATC: L01CD04

No doses: the clinician sets them by the current guideline.

Mechanism of action

β-tubulin (taxane site, inside the microtubule)Cabazitaxel

No public structure shows cabazitaxel on tubulin. The figure shows paclitaxel, which occupies the same taxane site, on bovine α/β-tubulin.

Target in 3D: β-tubulin (taxane site, inside the microtubule). PDB structure 1JFF (RCSB PDB, public domain). View the structure at RCSB PDB

Cabazitaxel binds tubulin, promotes its assembly into microtubules and blocks their disassembly. The over-stable microtubules cannot form a working mitotic spindle or carry out interphase functions, so the cell dies. It is a poor substrate for the P-glycoprotein efflux pump, which helps it work in prostate cancer that has become resistant to docetaxel.

Cabazitaxel binds the taxane site on β-tubulin
Microtubules are frozen: they assemble but cannot come apart
Mitosis fails and the cell dies

Indications

Metastatic castration-resistant prostate cancer previously treated with a docetaxel regimen, together with prednisone. Prostate cancer →

Adverse effects

Common

Diarrhoea, nausea, vomiting, abdominal pain
Tiredness, weakness, anaemia
Taste changes, loss of appetite, mouth sores
Numbness or tingling in the hands and feet
Blood in the urine; joint, back and muscle pain

Contraindications

Low neutrophil count
History of severe allergy to cabazitaxel or to drugs made with polysorbate 80
Severe liver impairment

Key interactions

Strong CYP3A inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, voriconazole): Raise cabazitaxel levels; the combination is avoided, or the dose is lowered if it cannot be.
St John's wort and other strong CYP3A inducers: Can lower cabazitaxel levels.
Aspirin and other NSAIDs: Add to the risk of gastrointestinal bleeding.

What is monitored

Blood count often, especially before each cycle
Vital signs and breathing during the infusion
Fluid balance, stools and kidney function
Liver tests (bilirubin) before treatment

Administration and safety

Premedication with an antihistamine, a corticosteroid and an H2 blocker is given before each infusion.
Diluted exactly as the product instructions state; given through non-PVC equipment with an in-line filter.
Given in a facility where an allergic reaction can be treated at once; the infusion is stopped if one occurs.
Hazardous drug: prepared and disposed of under cytotoxic-drug procedures.

Pregnancy and breastfeeding

Used only in men; it may harm a fetus, so men with partners who could become pregnant use contraception during treatment and for months after. It may lower male fertility.

Nursing care

Check the neutrophil count before each cycle; growth factor support may be ordered.
Watch closely during the first infusions for rash, flushing, low blood pressure or wheeze.
Teach to report fever, severe diarrhoea, blood in stool or urine, and less urine.
Ask about pelvic radiotherapy, NSAIDs, St John's wort and grapefruit.

Pharmacokinetics

Absorption: Intravenous infusion over about an hour.
Distribution: Very large volume of distribution; highly bound to albumin and lipoproteins.
Metabolism: Extensively in the liver, mainly by CYP3A4/5 and less by CYP2C8.
Elimination: Mostly in the faeces as metabolites; very little in the urine.
Half-life: Long terminal half-life, about 95 hours.

Test yourself

Think of the answer, then tap the question to see it.

When is cabazitaxel used in prostate cancer?

In metastatic castration-resistant disease already treated with docetaxel, together with prednisone.

Which excipient allergy is a contraindication to cabazitaxel?

Polysorbate 80.

Why might cabazitaxel work after docetaxel has failed?

It is a poor substrate for the P-glycoprotein efflux pump, a common cause of taxane resistance.

Which premedications are given before each cabazitaxel infusion?

An antihistamine, a corticosteroid and an H2 blocker.

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Connections

← Back to the class: Microtubule inhibitors

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: DailyMed - CABAZITAXEL kit (DailyMed (U.S. National Library of Medicine), 2021); Cabazitaxel Injection: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2025); Refined structure of alpha-beta tubulin from zinc-induced sheets stabilized with taxol (RCSB Protein Data Bank, 2001).

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Representative model, for educational purposes only.