Cabazitaxel
drugOn this page
Also known as Cabazitaxel accordCabazitaxel acetonateJevtanaJevtana kitNSC-761432TXD 258TXD-258TXD258XRP 6258XRP-6258XRP6258Cabazitaxel
Summary
Cabazitaxel (CHEMBL1201748) is an approved small-molecule antineoplastic agent (ATC L01CD04) targeting TUBB; indicated across 25 conditions including neoplasm and prostate carcinoma; with CIViC clinical evidence for 3 variant-indication associations (e.g. AR AR-V7 in prostate cancer).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01CD04
- Targets: 1 (TUBB)
- Indications: 25 conditions
- Clinical trials: 109
- Precision-oncology evidence (CIViC): 3 variant–indication associations
- Chemistry: 835.9 Da · C45H57NO14
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1201748 |
| Name | Cabazitaxel |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 9854073 |
| ChEBI | CHEBI:63584 |
| ATC | L01CD04 |
| Molecular formula | C45H57NO14 |
| Molecular weight | 835.9 |
| InChIKey | BMQGVNUXMIRLCK-OAGWZNDDSA-N |
SMILES: CC1=C2[C@H](C(=O)[C@@]3([C@H](C[C@@H]4[C@]([C@H]3[C@@H]([C@@](C2(C)C)(C[C@@H]1OC(=O)[C@@H]([C@H](C5=CC=CC=C5)NC(=O)OC(C)(C)C)O)O)OC(=O)C6=CC=CC=C6)(CO4)OC(=O)C)OC)C)OC
IUPAC name: [(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4-acetyloxy-1-hydroxy-15-[(2R,3S)-2-hydroxy-3-[(2-methylpropan-2-yl)oxycarbonylamino]-3-phenylpropanoyl]oxy-9,12-dimethoxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.03,10.04,7]heptadec-13-en-2-yl] benzoate
ChEBI definition: A tetracyclic diterpenoid that is 10-deacetylbaccatin III having O-methyl groups attached at positions 7 and 10 as well as an O-(2R,3S)-3-[(tert-butoxycarbonyl)amino]-2-hydroxy-3-phenylpropanoyl group attached at position 13. Acts as a microtubule inhibitor, binds tubulin and promotes microtubule assembly and simultaneously inhibits disassembly.
Pharmacological roles (ChEBI): antineoplastic agent, microtubule-stabilising agent.
Also known as: Cabazitaxel, Cabazitaxel accord, Cabazitaxel acetonate, Jevtana, Jevtana kit, NSC-761432, TXD 258, TXD-258, TXD258, XRP 6258, XRP-6258, XRP6258
Patent coverage: 3,901 distinct patent families (8,809 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| TUBB | tubulin beta class I | Inhibition | P07437 |
Bioactivity
No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).
Target pathways
Aggregated over 1 target gene(s): TUBB.
Top Reactome pathways
24 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Cell Cycle | 1 | TUBB |
| Disease | 1 | TUBB |
| Innate Immune System | 1 | TUBB |
| Immune System | 1 | TUBB |
| Organelle biogenesis and maintenance | 1 | TUBB |
| Regulation of PLK1 Activity at G2/M Transition | 1 | TUBB |
| Loss of Nlp from mitotic centrosomes | 1 | TUBB |
| Recruitment of mitotic centrosome proteins and complexes | 1 | TUBB |
| Loss of proteins required for interphase microtubule organization from the centrosome | 1 | TUBB |
| Centrosome maturation | 1 | TUBB |
| Recruitment of NuMA to mitotic centrosomes | 1 | TUBB |
| Mitotic G2-G2/M phases | 1 | TUBB |
| Cilium Assembly | 1 | TUBB |
| Anchoring of the basal body to the plasma membrane | 1 | TUBB |
| Infectious disease | 1 | TUBB |
| Neutrophil degranulation | 1 | TUBB |
| Mitotic Prometaphase | 1 | TUBB |
| M Phase | 1 | TUBB |
| G2/M Transition | 1 | TUBB |
| Cell Cycle, Mitotic | 1 | TUBB |
| AURKA Activation by TPX2 | 1 | TUBB |
| Potential therapeutics for SARS | 1 | TUBB |
| SARS-CoV Infections | 1 | TUBB |
| Viral Infection Pathways | 1 | TUBB |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| microtubule cytoskeleton organization | 1 |
| mitotic cell cycle | 1 |
| microtubule-based process | 1 |
| cytoskeleton-dependent intracellular transport | 1 |
| natural killer cell mediated cytotoxicity | 1 |
| regulation of synapse organization | 1 |
| spindle assembly | 1 |
| cell division | 1 |
| odontoblast differentiation | 1 |
| cytoskeleton organization | 1 |
Indications & clinical
Indications
25 indications (7 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| neoplasm | 4 | MONDO:0005070 | EFO:0000616 |
| prostate carcinoma | 4 | MONDO:0005159 | EFO:0001663 |
| prostate adenocarcinoma | 4 | MONDO:0005082 | EFO:0000673 |
| metastatic prostate carcinoma | 4 | MONDO:0004956 | EFO:0000196 |
| prostate cancer | 4 | MONDO:0008315 | MONDO:0008315 |
| dedifferentiated liposarcoma | 2 | MONDO:0020563 | EFO:0003085 |
| small cell lung carcinoma | 2 | MONDO:0008433 | EFO:0000702 |
| head and neck squamous cell carcinoma | 2 | MONDO:0010150 | EFO:0000181 |
| glioblastoma | 2 | MONDO:0018177 | EFO:0000519 |
| non-small cell lung carcinoma | 2 | MONDO:0005233 | EFO:0003060 |
| testicular cancer | 2 | MONDO:0005447 | EFO:0005088 |
| head and neck cancer | 2 | MONDO:0005627 | EFO:0006859 |
| transitional cell carcinoma | 2 | MONDO:0006474 | EFO:1000601 |
| penile neoplasm | 2 | MONDO:0006895 | EFO:1001094 |
| urothelial carcinoma | 2 | MONDO:0040679 | EFO:0008528 |
| adrenal cortex carcinoma | 2 | MONDO:0006639 | EFO:1000796 |
| gastric neoplasm | 2 | MONDO:0021085 | MONDO:0001056 |
| breast neoplasm | 2 | MONDO:0021100 | MONDO:0007254 |
| ovarian cancer | 2 | MONDO:0008170 | MONDO:0008170 |
| colorectal neoplasm | 2 | MONDO:0005335 | MONDO:0005575 |
| central nervous system cancer | 1 | MONDO:0002714 | EFO:0000326 |
| brain cancer | 1 | MONDO:0001657 | MONDO:0001657 |
3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 109.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 60 |
| PHASE3 | 14 |
| PHASE1 | 14 |
| PHASE1/PHASE2 | 11 |
| PHASE4 | 4 |
| PHASE2/PHASE3 | 4 |
| Not specified | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT01649635 | PHASE4 | COMPLETED | Study of Cabazitaxel Combined With Prednisone and Prophylaxis of Neutropenia Complications in the Treatment of Patients With Metastatic Castration-resistant Prostate Cancer |
| NCT02074137 | PHASE4 | COMPLETED | Evaluation of Safety of Cabazitaxel (Jevtana) in Patients With Metastatic Hormone Refractory Prostate Cancer |
| NCT02441894 | PHASE4 | COMPLETED | Combination of Cabazitaxel With Prednisolone With Primary Prophylaxis With PEG-G-CSF in Treatment of Patients With Prostate Cancer |
| NCT02485691 | PHASE4 | COMPLETED | Cabazitaxel Versus the Switch to Alternative AR-targeted Agent (Enzalutamide or Abiraterone) in Metastatic Castration-resistant Prostate Cancer (mCRPC) Patients Previously Treated With Docetaxel and Who Rapidly Failed a Prior AR-targeted Agent |
| NCT01952223 | PHASE3 | ACTIVE_NOT_RECRUITING | A Phase III of Cabazitaxel and Pelvic Radiotherapy in Localized Prostate Cancer and High-risk Features of Relapse |
| NCT03258320 | PHASE2/PHASE3 | RECRUITING | A Randomised Trial of Cabazitaxel, Docetaxel, Mitoxantrone or Satraplatin (CDMS) Plus Surgery for Prostate Cancer Patients |
| NCT06470243 | PHASE3 | RECRUITING | Testing Whether the Addition of Carboplatin Chemotherapy to Cabazitaxel Chemotherapy Will Improve Outcomes Compared to Cabazitaxel Alone in People With Castrate-Resistant Prostate Cancer That Has Spread Beyond the Prostate to Other Parts of the Body |
| NCT06691984 | PHASE3 | ACTIVE_NOT_RECRUITING | Phase 3 Study of Xaluritamig vs Cabazitaxel or Second Androgen Receptor-Directed Therapy in Participants With Progressive Metastatic Castration-Resistant Prostate Cancer (XALute) |
| NCT07213674 | PHASE3 | RECRUITING | A Study of Xaluritamig Plus Abiraterone Versus Investigator’s Choice in Participants With Chemotherapy-naïve Metastatic Castration-resistant Prostate Cancer |
| NCT07611110 | PHASE3 | RECRUITING | AZD2265 Compared With Standard of Care in PSMA-positive Metastatic Castration-resistant Prostate Cancer (VECTRA-01) |
| NCT00417079 | PHASE3 | COMPLETED | XRP6258 Plus Prednisone Compared to Mitoxantrone Plus Prednisone in Hormone Refractory Metastatic Prostate Cancer |
| NCT01083615 | PHASE3 | TERMINATED | A Study Evaluating the Pain Palliation Benefit of Adding Custirsen to Docetaxel Retreatment or Cabazitaxel as Second Line Therapy in Men With Metastatic Castrate Resistant Prostate Cancer (mCRPC) |
| NCT01254279 | PHASE3 | COMPLETED | Early Access to Cabazitaxel in Patients With Metastatic Hormone Refractory Prostate Cancer Previously Treated With a Docetaxel-containing Regimen |
| NCT01308567 | PHASE3 | COMPLETED | Cabazitaxel Versus Docetaxel Both With Prednisone in Patients With Metastatic Castration Resistant Prostate Cancer |
| NCT01308580 | PHASE3 | COMPLETED | Cabazitaxel at 20 mg/m² Compared to 25 mg/m² With Prednisone for the Treatment of Metastatic Castration Resistant Prostate Cancer |
| NCT01578655 | PHASE3 | COMPLETED | Comparison of Cabazitaxel/Prednisone Alone or in Combination With Custirsen for 2nd Line Chemotherapy in Prostate Cancer |
| NCT01668459 | PHASE2/PHASE3 | COMPLETED | Treatment of Locally Advanced or Metastatic Transitional Cell Carcinoma With Cabazitaxel |
| NCT01830231 | PHASE2/PHASE3 | UNKNOWN | Cabazitaxel vs. Vinflunine in Metastatic or Locally Advanced Transitional Cell Carcinoma of the Urothelium (TCCU) |
| NCT01978873 | PHASE3 | UNKNOWN | Efficacy Study Evaluating Chemotherapy in Prostate Cancer |
| NCT02044354 | PHASE3 | COMPLETED | Patient Preference Between Cabazitaxel and Docetaxel in Metastatic Castrate-resistant Prostate Cancer |
| NCT02961257 | PHASE3 | COMPLETED | Trial Evaluating the Safety of 2 Schedules of Cabazitaxel in Elderly Men With mCRPC Previously Treated With a Docetaxel |
| NCT03295565 | PHASE2/PHASE3 | COMPLETED | Optimal Sequencing of Treatment Options for Poor Risk mCRPC Previously Treated With Docetaxel |
| NCT02202772 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | Intravesical Cabazitaxel, Gemcitabine, and Cisplatin (CGC) in the Treatment Urothelial Carcinoma of the Bladder |
| NCT02522715 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | Enzalutamide and Cabazitaxel in Treating Patients With Metastatic, Castration-Resistant Prostate Cancer |
| NCT02703623 | PHASE2 | ACTIVE_NOT_RECRUITING | Abiraterone Acetate, Prednisone, and Apalutamide With or Without Ipilimumab or Cabazitaxel and Carboplatin in Treating Patients With Metastatic Castration-Resistant Prostate Cancer |
| NCT03263650 | PHASE2 | ACTIVE_NOT_RECRUITING | Study of Olaparib Maintenance Following Cabazitaxel-Carbo in Men With AVPC |
| NCT03419234 | PHASE2 | ACTIVE_NOT_RECRUITING | Abiraterone Acetate and Antiandrogen Therapy With or Without Cabazitaxel and Prednisone in Treating Patients With Metastatic, Castration-Resistant Prostate Cancer Previously Treated With Docetaxel |
| NCT04592237 | PHASE2 | ACTIVE_NOT_RECRUITING | Cabazitaxel, Carboplatin, and Cetrelimab Followed by Niraparib With or Without Cetrelimab for the Treatment of Aggressive Variant Metastatic Prostate Cancer |
| NCT04709276 | PHASE2 | ACTIVE_NOT_RECRUITING | A Study of Chemoimmunotherapy for the Treatment of Men With Neuroendocrine or Aggressive Variant Metastatic Prostate Cancer |
| NCT05340374 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | Cabazitaxel in Combination With 177Lu-PSMA-617 in Metastatic Castration-resistant Prostate Cancer |
| NCT05563558 | PHASE2 | RECRUITING | Pembrolizumab, Carboplatin and Cabazitaxel in Aggressive Metastatic Castration Resistant Prostate Cancer (PEAPOD_FOS) |
| NCT06085729 | PHASE1/PHASE2 | RECRUITING | Phase I/II Study of PEGylated Arginine Deiminase (ADI-PEG20) With Carboplatin and Cabazitaxel in Men With Aggressive Variant Prostate Cancers (AVPC) |
| NCT06353386 | PHASE1/PHASE2 | RECRUITING | Substudy 01A: Safety and Efficacy of Opevesostat (MK-5684)-Based Treatment Combinations or Opevesostat Alone in Participants With Metastatic Castration-resistant Prostate Cancer (mCRPC) (MK-5684-01A) |
| NCT06632977 | PHASE2 | RECRUITING | Targeted Treatment for Metastatic Prostate Cancer, The PREDICT Trial |
| NCT06738303 | PHASE2 | RECRUITING | Cabazitaxel +/- Carboplatin vs 177Lu-PSMA-617 in Metastatic Castrate-resistant Prostate Cancer |
| NCT06890832 | PHASE2 | NOT_YET_RECRUITING | A Study to Investigate Efficacy and Safety of Different Dose Regimen of Oral Cabazitaxel Tablet in Adult Participants with Prostate Cancer |
| NCT01001221 | PHASE1/PHASE2 | TERMINATED | Dose-Escalation, Safety, Pharmacokinetics Study of Cabazitaxel With Gemcitabine In Patients With Solid Tumor |
| NCT01365130 | PHASE2 | TERMINATED | Chemotherapy for Patients With Gastroesophageal Cancers Who Have Progressed After One Prior Chemo Regimen |
| NCT01437488 | PHASE2 | COMPLETED | Cabazitaxel in Patients With Urothelial Carcinoma Who Have Disease Progression Following Platinum-Based Chemotherapy |
| NCT01469338 | PHASE2 | TERMINATED | Cabazitaxel Plus Prednisone With Octreotide For Castration-Resistant Prostate Cancer (CRPC) Previously Treated With Docetaxel |
Clinical evidence (CIViC)
Variant × indication × effect (3 predictive associations from 3 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| AR AR-V7 | Prostate Cancer | Resistance | Cabazitaxel | CIViC B | EID9552 |
| IGF2 Overexpression | Prostate Cancer | Sensitivity/Response | Cabazitaxel + Linsitinib | CIViC D | EID12428 |
| IGF2 Overexpression | Prostate Cancer | Sensitivity/Response | Docetaxel + Cabazitaxel + Linsitinib | CIViC D | EID414 |
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 11 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
18 molecules share ≥1 primary target. Top 18 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| PODOFILOX | ChEMBL + PubChem | Phase 4 (approved) | TUBB |
| VINBLASTINE | ChEMBL + PubChem | Phase 4 (approved) | TUBB |
| COLCHICINE | ChEMBL | Phase 4 (approved) | TUBB |
| DOCETAXEL | ChEMBL | Phase 4 (approved) | TUBB |
| LEVOFLOXACIN | ChEMBL | Phase 4 (approved) | TUBB |
| NOSCAPINE | ChEMBL | Phase 4 (approved) | TUBB |
| PACLITAXEL | ChEMBL | Phase 4 (approved) | TUBB |
| TIRBANIBULIN | ChEMBL | Phase 4 (approved) | TUBB |
| VINCRISTINE | ChEMBL | Phase 4 (approved) | TUBB |
| VINORELBINE | ChEMBL | Phase 4 (approved) | TUBB |
| PATUPILONE | ChEMBL | Phase 3 | TUBB |
| ABT-751 | ChEMBL | Phase 2 | TUBB |
| DOLASTATIN-10 | ChEMBL | Phase 2 | TUBB |
| INDIBULIN | ChEMBL | Phase 2 | TUBB |
| MAYTANSINE | ChEMBL | Phase 2 | TUBB |
| MOLIBRESIB | ChEMBL | Phase 2 | TUBB |
| NOCODAZOLE | ChEMBL | Phase 2 | TUBB |
| PARBENDAZOLE | ChEMBL | Phase 2 | TUBB |
Related Atlas pages
- Genes: TUBB
- Diseases: neoplasm, prostate carcinoma, prostate adenocarcinoma, metastatic prostate carcinoma, prostate cancer
- Drugs: Podofilox, Vinblastine, Colchicine, Docetaxel, Levofloxacin, Noscapine, Paclitaxel, Tirbanibulin, Vincristine, Vinorelbine, Patupilone
- Biomarker genes: FDXR