Iniparib

Summary

Iniparib (CHEMBL1170047) is a phase-3 clinical-stage small molecule; indicated across 6 conditions including neoplasm and squamous cell lung carcinoma; with CIViC clinical evidence for 1 variant-indication association (e.g. BRCA2 Mutation in pancreatic cancer).

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 6 conditions
• Clinical trials: 17
• Precision-oncology evidence (CIViC): 1 variant–indication association
• Chemistry: 292.03 Da · C7H5IN2O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1170047
Name	Iniparib
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	9796068
Molecular formula	C7H5IN2O3
Molecular weight	292.03
InChIKey	MDOJTZQKHMAPBK-UHFFFAOYSA-N

SMILES: C1=CC(=C(C=C1C(=O)N)[N+](=O)[O-])I

IUPAC name: 4-iodo-3-nitrobenzamide

Also known as: BSI-201, Iniparib, Sar-240550, SAR240550, INIPARIB, SID137275940, INIPARIB (BSI-201), IniparibÊ, Iniparib (BSI-201), IniparibÂ, C0088785

Patent coverage: 1,216 distinct patent families (3,007 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 2,445 (81%) 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

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Poly [ADP-ribose] polymerase 1.

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

6 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	3	MONDO:0005070	EFO:0000616
squamous cell lung carcinoma	3	MONDO:0005097	EFO:0000708
breast neoplasm	3	MONDO:0021100	MONDO:0007254
non-small cell lung carcinoma	2	MONDO:0005233	EFO:0003060
uterine carcinosarcoma	2	MONDO:0006485	EFO:1000613
ovarian cancer	2	MONDO:0008170	MONDO:0008170

Clinical trials

Total trials: 17.

Phase distribution

Phase	Trials
PHASE2	9
PHASE1	5
PHASE3	2
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00938652	PHASE3	COMPLETED	A Phase 3, Multi-Center Study of Gemcitabine/Carboplatin, With or Without BSI-201, in Patients With ER-, PR-, and Her2-Negative Metastatic Breast Cancer
NCT01593228	PHASE3	COMPLETED	Treatment Extension Study for Patients Who Have Previously Participated and Have Benefited From Iniparib in a Clinical Trial
NCT00540358	PHASE2	COMPLETED	A Phase 2 Trial of Standard Chemotherapy, With or Without BSI-201, in Patients With Triple Negative Metastatic Breast Cancer
NCT00677079	PHASE2	COMPLETED	Single Arm Study of BSI-201 in Patients With BRCA-1 or BRCA-2 Associated Advanced Epithelial Ovarian, Fallopian Tube, or Primary Peritoneal Cancer
NCT00687687	PHASE2	COMPLETED	Evaluation of Paclitaxel (Taxol, NSC #673089), Carboplatin (Paraplatin, NSC #241240), and BSI-201 (NSC #746045, IND #71,677) in the Treatment of Advanced, Persistent, or Recurrent Uterine Carcinosarcoma
NCT01033123	PHASE2	COMPLETED	A Single-Arm Study Evaluating Carboplatin/Gemcitabine in Combination With BSI-201 in Patients With Platinum-Sensitive Recurrent Ovarian Cancer
NCT01033292	PHASE2	COMPLETED	A Single-Arm Study Evaluating Carboplatin/Gemcitabine in Combination With BSI-201 in Patients With Platinum-Resistant Recurrent Ovarian Cancer
NCT01045304	PHASE2	COMPLETED	Study of SAR240550 (BSI-201) in Combination With Gemcitabine/Carboplatin, in Patients With Metastatic Triple Negative Breast Cancer
NCT01086254	PHASE2	COMPLETED	SAR240550 in Combination With Gemcitabine/Cisplatin in Non-small Cell Lung Cancer
NCT01173497	PHASE2	COMPLETED	A Study Evaluating INIPARIB in Combination With Chemotherapy to Treat Triple Negative Breast Cancer Brain Metastasis
NCT01204125	PHASE2	COMPLETED	Two Regimens of SAR240550/Weekly Paclitaxel and Paclitaxel Alone as Neoadjuvant Therapy in Triple Negative Breast Cancer Patients
NCT00298675	PHASE1	COMPLETED	Phase 1/1b Dose Escalation Study Evaluating BSI-201 as a Single Agent and in Combination With Irinotecan in Subjects With Advanced Solid Tumors
NCT00422682	PHASE1	COMPLETED	A Study Evaluating BSI-201 in Combination With Chemotherapeutic Regimens in Subjects With Advanced Solid Tumors
NCT01161836	PHASE1	COMPLETED	An Open-label Study Investigating the Disposition and QT/QTc Interval Effects of 400 mg [14C]-Iniparib(3.7 MBq, 100 µCi)
NCT01213381	PHASE1	COMPLETED	Safety and Pharmacokinetics of SAR240550 (BSI-201) Twice Weekly in Patients With Advanced Solid Tumors
NCT01455532	PHASE1	COMPLETED	A Dose Escalation Study of Iniparib as a Single Agent and in Combination in Solid Tumors
NCT01130259	Not specified	NO_LONGER_AVAILABLE	An Open-Label, Expanded Access Protocol of Iniparib Breast Cancer

Clinical evidence (CIViC)

Variant × indication × effect (1 predictive associations from 1 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
BRCA2 Mutation	Pancreatic Cancer	Sensitivity/Response	Iniparib	CIViC C	EID5936

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

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