Tesetaxel

Summary

Tesetaxel (CHEMBL2107787) is a phase-3 clinical-stage small molecule; indicated across 6 conditions including breast neoplasm and melanoma.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 6 conditions
• Clinical trials: 12
• Chemistry: 882 Da · C46H60FN3O13

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2107787
Name	Tesetaxel
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	6918574
Molecular formula	C46H60FN3O13
Molecular weight	882
InChIKey	MODVSQKJJIBWPZ-VLLPJHQWSA-N

SMILES: CC1=C2[C@@H]3[C@H]([C@@]4(CC[C@@H]5[C@]([C@H]4[C@@H]([C@@](C2(C)C)(C[C@@H]1OC(=O)[C@@H]([C@H](C6=C(C=CC=N6)F)NC(=O)OC(C)(C)C)O)O)OC(=O)C7=CC=CC=C7)(CO5)OC(=O)C)C)O[C@@H](O3)CN(C)C

IUPAC name: [(2R,4S,6S,7R,10R,13S,14R,15S,16S,18S)-13-acetyloxy-4-[(dimethylamino)methyl]-18-[(2R,3S)-3-(3-fluoro-2-pyridinyl)-2-hydroxy-3-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]oxy-16-hydroxy-7,19,20,20-tetramethyl-3,5,11-trioxapentacyclo[14.3.1.02,6.07,14.010,13]icos-1(19)-en-15-yl] benzoate

Also known as: Tesetaxel, TESETAXEL

Patent coverage: 1,173 distinct patent families (3,042 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 2,821 (93%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

No target linkage available.

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

4 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
breast neoplasm	3	MONDO:0021100	EFO:0003869
melanoma	2	MONDO:0005105	EFO:0000756
gastric carcinoma	2	MONDO:0004950	EFO:0000178
neoplasm	1	MONDO:0005070	EFO:0000616

2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 12.

Phase distribution

Phase	Trials
PHASE2	9
PHASE1	2
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03326674	PHASE3	TERMINATED	Tesetaxel Plus Reduced Dose of Capecitabine vs. Capecitabine in HER2 Negative, HR Positive, LA/MBC
NCT01064713	PHASE2	COMPLETED	Phase II Study of Tesetaxel in Metastatic Melanoma
NCT01092585	PHASE2	UNKNOWN	Tesetaxel as Second-line Therapy for Patients With Advanced Melanoma and Normal Serum LDH
NCT01095120	PHASE2	UNKNOWN	Tesetaxel as Second-line Therapy for Patients With Advanced Gastric Cancer
NCT01215877	PHASE2	UNKNOWN	Tesetaxel for Previously Treated Patients With Bladder Cancer
NCT01296243	PHASE2	UNKNOWN	Tesetaxel in Chemotherapy-naive Patients With Progressive, Castration-resistant Prostate Cancer
NCT01573468	PHASE2	UNKNOWN	Capecitabine/Tesetaxel Versus Capecitabine/Placebo as Second-line Therapy for Gastric Cancer
NCT01609127	PHASE2	UNKNOWN	Tesetaxel Every 3 Weeks vs Weekly vs Capecitabine as 1st-line Therapy for Locally Advanced or Metastatic Breast Cancer
NCT03858972	PHASE2	TERMINATED	Tesetaxel Plus Reduced Dose of Capecitabine in Patients With HER2 Negative, HR Positive, LA/MBC
NCT03952325	PHASE2	TERMINATED	Tesetaxel Plus 3 Different PD-(L)1 Inhibitors in Patients With Triple-Negative MBC and Tesetaxel Monotherapy in Patients With HER2-Negative MBC
NCT01337310	PHASE1	UNKNOWN	Study of Tesetaxel in Japanese Patients With Solid Tumors
NCT04312282	PHASE1	TERMINATED	The Effect of Tesetaxel on the QTc Interval and the Effect of Food, Itraconazole, and Rifampin on Tesetaxel Pharmacokinetics in Patients With Advanced Solid Tumors

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).