Iniparib - CAS 160003-66-7
Catalog number: 160003-66-7
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
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Targets:
PARP
Description:
BSI-201 is a small-molecule prodrug inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase-1 (PARP-1) with potential chemosensitizing, radiosensitizing and antineoplastic activities. In vivo, PARP-1 inhibitor BSI-201 is converted to the active drug, which selectively binds to PARP-1 and inhibits PARP-1- mediated DNA repair. Consequently, this agent may enhance the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy and radiation therapy. In addition, PARP-1 inhibitor BSI-201 may exhibit direct antineoplastic activity against cancers defective in DNA repair. PARP-1 catalyzes post-translational ADP-ribosylation of nuclear proteins and is activated by single-strand DNA (ssDNA) breaks.
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Synonyms:
BSI-201; NSC-746045; IND-71677. Iniparib
MSDS:
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Current Developer:
BiPar Sciences
1.A Phase 2, Single Arm Study of Iniparib in Patients With BRCA1 or BRCA2 Associated Advanced Epithelial Ovarian, Fallopian Tube, or Primary Peritoneal Cancer.
Bell-McGuinn KM1, Konner JA, Tew WP, Hensley ML, Iasonos A, Charpentier E, Mironov S, Sabbatini P, Aghajanian C. Int J Gynecol Cancer. 2016 Feb;26(2):255-60. doi: 10.1097/IGC.0000000000000591.
OBJECTIVE: The aim of the study was to evaluate the activity and tolerability of iniparib monotherapy in women with BRCA1 or BRCA2-associated advanced epithelial ovarian, fallopian tube, or primary peritoneal cancer.
2.SOLTI NeoPARP: a phase II randomized study of two schedules of iniparib plus paclitaxel versus paclitaxel alone as neoadjuvant therapy in patients with triple-negative breast cancer.
Llombart-Cussac A1,2, Bermejo B3,4, Villanueva C3,5, Delaloge S6, Morales S3,7, Balmaña J3,8, Amillano K3,9, Bonnefoi H10, Casas A3,11, Manso L3,12, Roché H13, Gonzalez-Santiago S3,14, Gavilá J3,15, Sánchez-Rovira P16, Di Cosimo S3,17, Harbeck N18, Charpe Breast Cancer Res Treat. 2015 Nov;154(2):351-7. doi: 10.1007/s10549-015-3616-8. Epub 2015 Nov 4.
Iniparib is an investigational agent with antitumor activity of controversial mechanism of action. Two previous trials in advanced triple-negative breast cancer (TNBC) in combination with gemcitabine and carboplatin showed some evidence of efficacy that was not confirmed. This phase II randomized neoadjuvant study was designed to explore its activity and tolerability with weekly paclitaxel (PTX) as neoadjuvant treatment in TNBC patients. 141 patients with Stage II-IIIA TNBC were randomly assigned to receive PTX (80 mg/m(2), d1; n = 47) alone or in combination with iniparib, either once-weekly (PWI) (11.2 mg/kg, d1; n = 46) or twice-weekly (PTI) (5.6 mg/kg, d1, 4; n = 48) for 12 weeks. Primary endpoint was pathologic complete response (pCR) in the breast. pCR rate was similar among the three arms (21, 22, and 19 % for PTX, PWI, and PTI, respectively). Secondary efficacy endpoints were comparable: pCR in breast and axilla (21, 17, and 19 %); best overall response in the breast (60, 61, and 63 %); and breast conservation rate (53, 54, and 50 %).
3.Phase I study of iniparib concurrent with monthly or continuous temozolomide dosing schedules in patients with newly diagnosed malignant gliomas.
Blakeley JO1, Grossman SA2, Mikkelsen T3, Rosenfeld MR4, Peereboom D5, Nabors LB6, Chi AS7, Emmons G8, Garcia Ribas I8, Supko JG7, Desideri S2, Ye X2. J Neurooncol. 2015 Oct;125(1):123-31. doi: 10.1007/s11060-015-1876-0. Epub 2015 Aug 19.
Iniparib is a prodrug that converts to highly reactive cytotoxic metabolites intracellularly with activity in preclinical glioma models. We investigated the maximum tolerated dose (MTD) of iniparib with monthly (m) and continuous (c) temozolomide (TMZ) dosing schedules in patients with malignant gliomas (MG). Adults with newly diagnosed MG who had successfully completed ≥80% of radiation (RT) and TMZ without toxicity received mTMZ dosing (150-200 mg/m(2) days 1-5/28 days) or cTMZ dosing (75 mg/m(2)/days × 6 weeks) in conjunction with iniparib (i.v. 2 days/week) in the adjuvant setting. Iniparib was dose escalated using a modified continual reassessment method (mCRM). 43 patients (32 male; 34 GBM, 8 AA, 1 gliosarcoma; median age 54 years; median KPS 90) were enrolled across 4 dose levels. In the mTMZ group, 2/4 patients had dose limiting toxicities (DLT) at 19 mg/kg/week (rash/hypersensitivity). At 17.2 mg/kg/week, 1/9 patients had a DLT (grade 3 fatigue).
4.A Comparative Oncology Study of Iniparib Defines Its Pharmacokinetic Profile and Biological Activity in a Naturally-Occurring Canine Cancer Model.
Saba C1, Paoloni M2, Mazcko C2, Kisseberth W3, Burton JH4, Smith A5, Wilson-Robles H6, Allstadt S7, Vail D8, Henry C9, Lana S4, Ehrhart EJ4, Charles B4, Kent M7, Lawrence J1, Burgess K10, Borgatti A11, Suter S12, Woods P13, Gordon I2, Vrignaud P14, Khanna PLoS One. 2016 Feb 11;11(2):e0149194. doi: 10.1371/journal.pone.0149194. eCollection 2016.
Development of iniparib as an anti-cancer agent was hindered in part by lingering questions regarding its mechanism of action, the activity of its metabolites, and their potential accumulation in tumors. Due to strong similarities in metabolism of iniparib between humans and dogs, a veterinary clinical trial in pet dogs with spontaneous cancers was designed to answer specific questions pertaining to pharmacokinetic exposures and tolerability of iniparib. Dogs were treated with iniparib alone and in combination with carboplatin chemotherapy. Iniparib doses ranged between 10-70 mg/kg intravenously (IV). Plasma, tumor and normal tissue samples were collected before and at various time points scheduled after exposure for pharmacokinetic and biologic analysis. The primary endpoints included characterization of dose-limiting toxicities (DLT) and determination of the drug exposures that could be achieved in both normal and tumor tissues. Nineteen dogs were treated.
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CAS 160003-66-7 Iniparib

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