Iniparib

Iniparib
Systematic (IUPAC) name
4-iodo-3-nitrobenzamide
Clinical data
Pregnancy cat.  ?
Legal status Investigational
Identifiers
CAS number 160003-66-7 N
ATC code None
PubChem CID 9796068
ChemSpider 7971834 Y
UNII 2ZWI7KHK8F Y
KEGG D09913 N
ChEMBL CHEMBL1170047 Y
Chemical data
Formula C7H5IN2O3 
Mol. mass 292.03 g/mol
SMILES eMolecules & PubChem
 N(what is this?)  (verify)

Iniparib (previously BSI 201) (4-iodo-3-nitrobenzamide) is a drug that acts as an irreversible inhibitor of PARP1 (hence, it is a PARP inhibitor) and possibly other enzymes through covalent modification.[1][2] It is undergoing clinical trials for treatment of some types of breast cancer.[3][4]

It is the first PARP inhibitor to commence phase III clinical trials.[5] The first was for breast cancer,[6] another has started for squamous cell lung cancer.[7]

Preliminary results in June 2009 on triple-negative breast cancer were promising.[8] Later results showed increased median survival of triple negative breast cancer patients from 7.7 to 12.2 months.[9][10][11] However, Phase III results disclosed in January 2011 were disappointing.

Since December 2009, the FDA have been fast-tracking the New Drug Application of iniparib for triple-negative breast cancer.

References

  1. ^ http://www.cancernetwork.com/display/article/10165/1514773 "Development of PARP Inhibitors: An Unfinished Story " Jan 2010
  2. ^ http://www.biparsciences.com/000011.html
  3. ^ http://www.parp-inhibitors.com/bsi201.html
  4. ^ "New breast cancer drugs block cell repair enzyme". Reuters. 2009-05-31. http://www.reuters.com/article/healthNews/idUSTRE54U1FV20090531. 
  5. ^ "PARP Inhibitors in Oncology. Chemosensitizers or Single-Agent Therapeutics?". July 2009. http://www.p-d-r.com/ranking/Wolters%20Kluwer%20Health/July09/PARPi.WKHealth.29Jul09.pdf. 
  6. ^ "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". http://clinicaltrials.gov/ct2/show/NCT00938652.  2009 to 2012, Primary completion date June 2011
  7. ^ "Trial of Gemcitabine/Carboplatin With or Without BSI-201 (a PARP1 Inhibitor) in Patients With Previously Untreated Advanced Squamous Cell Lung Cancer (ECLIPSE)". http://clinicaltrials.gov/ct2/show/NCT01082549.  2010 to 2014, PCD 2012
  8. ^ "Sanofi’s new drug BSI 201 offers to treat the toughest breast cancer". 3 June 2009. http://www.dancewithshadows.com/pillscribe/sanofi%E2%80%99s-new-drug-bsi-201-offers-to-treat-the-toughest-breast-cancer/. 
  9. ^ "SABCS: PARP Inhibitor Data Called 'Spectacular'". Dec 2009. http://www.medpagetoday.com/MeetingCoverage/SABCS/17496. 
  10. ^ "PARP Inhibitor Adds Nearly 5 Months to Breast Cancer Survival". 11 Oct 2010. http://www.internalmedicinenews.com/news/oncology-hematology/single-article/parp-inhibitor-adds-nearly-5-months-to-breast-cancer-survival/5b8b2da248.html. 
  11. ^ O'Shaughnessy et al.; Osborne, Cynthia; Pippen, John E.; Yoffe, Mark; Patt, Debra; Rocha, Christine; Koo, Ingrid Chou; Sherman, Barry M. et al. (2011). "Iniparib plus Chemotherapy in Metastatic Triple-Negative Breast Cancer". New England Journal of Medicine 364 (3): 205–214. doi:10.1056/NEJMoa1011418. PMID 21208101. http://www.nejm.org/doi/full/10.1056/NEJMoa1011418.