Iniparib

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Structural formula
Structural formula of iniparib
General
Surname Iniparib
other names

4-iodo-3-nitrobenzamide

Molecular formula C 7 H 5 IN 2 O 3
External identifiers / databases
CAS number 160003-66-7
EC number 685-396-9
ECHA InfoCard 100.210.980
PubChem 9796068
ChemSpider 7971834
DrugBank DB13877
Wikidata Q260286
properties
Molar mass 292.03 g · mol -1
safety instructions
GHS labeling of hazardous substances
07 - Warning

Caution

H and P phrases H: 302-319
P: ?
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Iniparib (former name: BSI 201, manufacturer: Sanofi-Aventis ) is a substance that irreversibly inhibits the DNA- repairing protein PARP-1 (enzyme). It was in clinical trials for the treatment of various cancers , such as the lung cancer and the so-called triple receptor negative breast cancer ( triple-negative breast cancer , TNBC).

The initially promising results in terms of progression-free survival and overall survival after treatment for iniparib in triple receptor-negative breast cancer could not be confirmed in a large phase III study. That is why Sanofi stopped development of the active ingredient in 2013. This cost the group around € 219 million.

application areas

Iniparib is an anti-tumor agent with a poly (ADP-ribose) polymerase (PARP) -inhibiting effect. The enzyme PARP is an important regulator for the repair of DNA damage. By inhibiting PARP, the repair of DNA damage is prevented or made more difficult.

Side effects

Side effects include neutropenia , anemia , thrombocytopenia , asthenia , nausea, and constipation .

Individual evidence

  1. Template: CL Inventory / not harmonized There is not yet a harmonized classification for this substance . A label of [No public or meaningful name is available] in the Classification and Labeling Inventory of the European Chemicals Agency (ECHA), accessed on July 3, 2020, is reproduced from a self-classification by the distributor .
  2. Trial of Gemcitabine / Carboplatin With or Without BSI-201 (a PARP1 Inhibitor) in Patients With Previously Untreated Advanced Squamous Cell Lung Cancer (ECLIPSE) . Retrieved January 26, 2011. 2010 to 2014, PCD 2012.
  3. Joyce O'Shaughnessy et al., Iniparib plus Chemotherapy in Metastatic Triple-Negative Breast Cancer , In: The New England Journal of Medicine 2011; 364: 205-214, doi : 10.1056 / NEJMoa1011418 (free full text).
  4. Sanofi-Aventis, press release ( Memento of November 29, 2014 in the Internet Archive ) (PDF; 77 kB).
  5. a b ChemManager 11–12 / 2013: Sanofi stops drug development , GIT-Verlag Darmstadt.