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Billed as the first PARP inhibitor for triple-negative breast cancer, it failed its phase 3 in 2011. It turned out not to inhibit PARP at all.
A randomised phase 2 (O'Shaughnessy, NEJM 2011) in metastatic TNBC showed improved response, PFS, and OS when iniparib was added to gemcitabine-carboplatin. The phase 3 (n=519) missed both co-primary endpoints. Subsequent biochemistry showed iniparib does not trap or inhibit PARP1/2 at clinically relevant concentrations; it acts as a non-specific thiol-reactive compound. Sanofi (which had bought BiPar for up to $500M) discontinued it after a negative phase 3 in squamous NSCLC (2013).
Lesson: mechanism claims should be verified before a class label is attached; the true PARP inhibitors (olaparib, talazoparib) later succeeded in BRCA-mutant breast cancer.
Originally described as a PARP1 inhibitor; later shown to be a non-selective cysteine-modifying agent without PARP inhibition. Connects to PARP.
1.Iniparib slips into a pocket on PARP.
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Query for this drug: (TITLE:"Iniparib" OR ABSTRACT:"Iniparib" OR TITLE:"BSI-201" OR ABSTRACT:"BSI-201" OR TITLE:"SAR240550" OR ABSTRACT:"SAR240550") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Iniparib, not a curated reading list.
Shares Sanofi, Failures are hidden, Non-small-cell lung cancer and the tag failure.
Shares Failures are hidden and the tag failure.
Shares Failures are hidden and the tag failure.
Shares Failures are hidden and the tag failure.
Shares Failures are hidden and the tag failure.
Shares Failures are hidden, Non-small-cell lung cancer and the tag failure.
Shares Failures are hidden and the tag failure.
Shares Failures are hidden and the tag failure.