Palazestrant

Summary

Palazestrant (CHEMBL5314475) is a phase-3 clinical-stage small molecule; indicated across 3 conditions including neoplasm and breast carcinoma.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 3 conditions
• Clinical trials: 6
• Chemistry: 449.6 Da · C28H36FN3O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL5314475
Name	Palazestrant
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	135351887
Molecular formula	C28H36FN3O
Molecular weight	449.6
InChIKey	LBSFUBLFDCAEKV-XHCCPWGMSA-N

SMILES: CCCN1CC(C1)OC2=CC=C(C=C2)[C@@H]3C4=C(C[C@H](N3CC(C)(C)F)C)C5=CC=CC=C5N4

IUPAC name: (1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1-[4-(1-propylazetidin-3-yl)oxyphenyl]-1,3,4,9-tetrahydropyrido[3,4-b]indole

Also known as: Op-1250, OP-1250, Palazestrant, PALAZESTRANT, US11672785, Compound B

Patent coverage: 23 distinct patent families (50 SureChEMBL compound mentions), from 2 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

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

3 indications (0 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	2	MONDO:0005070	EFO:0000616
breast carcinoma	1	MONDO:0004989	EFO:0000305
breast neoplasm	1	MONDO:0021100	MONDO:0007254

Clinical trials

Total trials: 6.

Phase distribution

Phase	Trials
PHASE1	3
PHASE3	2
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06016738	PHASE3	RECRUITING	OP-1250 (Palazestrant) vs. Standard of Care for the Treatment of ER+/HER2- Advanced Breast Cancer
NCT07085767	PHASE3	RECRUITING	Palazestrant in Combination With Ribociclib for the First-line Treatment of ER+/HER2- Advanced Breast Cancer
NCT04505826	PHASE1/PHASE2	COMPLETED	A Dose Escalation/Expansion Study of Oral OP-1250 in Subjects With Advanced and/or Metastatic HR+, HER2- Breast Cancer
NCT05266105	PHASE1	ACTIVE_NOT_RECRUITING	A Phase 1 Study of Oral OP-1250 in Combination With Palbociclib in HR+/HER2- Breast Cancer Patients
NCT05508906	PHASE1	RECRUITING	Phase 1b Study of OP-1250 (Palazestrant) in Combination With Ribociclib, Alpelisib, Everolimus, or Atirmociclib in ER+, HER2- Breast Cancer
NCT06784193	PHASE1	RECRUITING	Phase 1 Study of OP-3136 in Advanced or Metastatic 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).