[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Microtubule inhibitors](https://durgical.com/en/pharmacology/classes/microtubule-inhibitors/) › Cabazitaxel

# 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](https://durgical.com/en/pharmacology/classes/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.

On this page

- The basics Mechanism of action
- Indications
- Adverse effects
- Pharmacokinetics
- Memory aid

- Clinical What the labels mean

- Safety Contraindications
- Key interactions
- What is monitored
- Administration and safety
- Pregnancy and breastfeeding
- Nursing care

- Study Test yourself

- Connections Connections

## 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](https://www.rcsb.org/structure/1JFF) · Drag to rotate · pinch to zoom

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 →](https://durgical.com/en/conditions/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

### Serious (rare, important)

- Severe neutropenia and febrile neutropenia, with deaths reported (more in people over 65)
- Severe allergic reactions (rash, low blood pressure, bronchospasm), mostly in the first infusions
- Severe diarrhoea with dehydration; gastrointestinal bleeding, perforation and neutropenic enterocolitis
- Kidney failure; cystitis and haematuria after pelvic radiotherapy
- Interstitial pneumonitis and acute respiratory distress

## 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.

## Memory aid

CABAZItaxel is the taxane that CAN BYPASS the pump (P-glycoprotein): the next step after docetaxel in prostate cancer. Count the neutrophils first.

## 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.

[Add to my cards (4)](https://durgical.app/estudiar/?add=/en/pharmacology/cabazitaxel/)

[More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology)

## What the labels mean

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

## Connections

## Related drugs 3

- [Docetaxel](https://durgical.com/en/pharmacology/docetaxel/)
- [Paclitaxel](https://durgical.com/en/pharmacology/paclitaxel/)
- [Abiraterone](https://durgical.com/en/pharmacology/abiraterone/)

## Related conditions 1

- [Prostate cancer](https://durgical.com/en/conditions/prostate-cancer/)

[← Back to the class: Microtubule inhibitors](https://durgical.com/en/pharmacology/classes/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](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ec6892c8-01e1-6a8b-e053-2995a90a956f) (DailyMed (U.S. National Library of Medicine), 2021); [Cabazitaxel Injection: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a611009.html) (MedlinePlus (U.S. National Library of Medicine), 2025); [Refined structure of alpha-beta tubulin from zinc-induced sheets stabilized with taxol](https://www.rcsb.org/structure/1JFF) (RCSB Protein Data Bank, 2001).

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Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/cabazitaxel/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/cabazitaxel/
