Delving into the Latest Updates on Iniparib with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

4-iodo-3-nitrobenzamide, Iniparib (USAN/INN), NIBA

+ [5]

Target

PARP1

Mechanism

PARP1 inhibitors(Poly (ADP-Ribose) polymerase 1 inhibitors)

Therapeutic Areas

NeoplasmsSkin and Musculoskeletal DiseasesNervous System Diseases+ [4]

Active Indication-

Inactive Indication

Advanced Malignant Solid NeoplasmBrain metastasesEstrogen receptor-negative breast cancer+ [13]

Originator Organization

Sanofi

Active Organization-

Inactive Organization

Sanofi

Drug Highest PhasePendingPhase 3

First Approval Date-

RegulationOrphan Drug (US)

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Structure/Sequence

Molecular FormulaC7H5IN2O3

InChIKeyMDOJTZQKHMAPBK-UHFFFAOYSA-N

CAS Registry160003-66-7

Primary Objective:
To assess the safety and the maximum tolerated dose(MTD) of iniparib as a single agent and in combination with chemotherapeutic regimens in patients with advanced solid tumors that are refractory to standard therapy.
Secondary Objectives:
To assess the antitumor effect of iniparib (per Response Evaluation Criteria in Solid Tumors [RECIST]) Version 1.1 in patients with measurable disease.
To characterize iniparib (and its metabolites, if possible) pharmacokinetics.
Based on data generated by Sanofi, it is concluded that iniparib does not possess characteristics typical of the PARP inhibitor class. The exact mechanism has not yet been fully elucidated, however based on experiments on tumor cells performed in the laboratory, iniparib is a novel investigational anti-cancer agent that induces gamma-H2AX (a marker of DNA damage) in tumor cell lines, induces cell cycle arrest in the G2/M phase in tumor cell lines, and potentiates the cell cycle effects of DNA damaging modalities in tumor cell lines. Investigations into potential targets of iniparib and its metabolites are ongoing.

Start Date01 Nov 2011

Sponsor / Collaborator

Sanofi

100 Clinical Results associated with Iniparib

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100 Translational Medicine associated with Iniparib

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100 Patents (Medical) associated with Iniparib

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181

Literatures (Medical) associated with Iniparib

17 Jan 2025·ORGANIC LETTERS

Polyfluoroalkanoic Acids as Fluoroalkylating Reagents: Strategy for Direct Access to R_f-Embedded Amides

Article

Author: Kabadwal, Lalit Mohan ; Bera, Atanu ; Haldar, Shuvojit ; Banerjee, Debasis

Herein, we have reported the application of bench stable perfluoroalkanoic acids as fluoro-alkylating reagents in combination with DIB and primary amides for sequential one-pot transformation to R_f-embedded functionalized amides under metal-free conditions. The protocol is tolerant to a range of sensitive functional groups (>33 examples and up to 90% yield), and perfluoro acids. Preliminary mechanistic studies, control experiments, in situ ¹⁹F-NMR analyses, and the synthesis of intermediate species were performed to understand the reaction pathways.

01 May 2024·Current medicinal chemistry

LIMD2 is the Signature of Cell Aging-immune/Inflammation in Acute Myocardial Infarction

Article

Author: Tao, Ping ; Feng, Jianyi ; Xu, Lei ; Nie, Qinqi ; Xu, Mujuan ; Chen, Junteng ; Chen, Xiaoming

Background::

Acute myocardial infarction (AMI) is an age-dependent cardiovascular disease in which cell aging, immunity, and inflammatory factors alter the course; however, cell aging-immune/inflammation signatures in AMI have not been investigated.

Methods::

Based on the GEO database to obtain microRNA (miRNA) sequencing, mRNA sequencing and single-cell sequencing data, and utilizing the Seurat package to identify AMI-associated cellular subpopulations. Subsequently, differentially expressed miRNAs and mRNAs were screened to establish a network of competing endogenous RNAs (ceRNAs). Senescence and immunity scores were calculated by single sample gene set enrichment analysis (ssGSEA), ESTIMATE and CIBERSORT algorithms, and the Hmisc package was used to screen for genes with the highest correlation with senescence and immunity scores. Finally, protein-protein interaction (PPI) and molecular docking analyses were performed to predict potential therapeutic agents for the treatment of AMI.

Results::

Four cell types (Macrophage, Fibroblast, Endothelial cells, CD8 T cells) were identified in AMI, and CD8 T cells exhibited the lowest cell aging activity. A ceRNA network of miRNAs- mNRA interactions was established based on the overlapping genes in differentially expressed miRNAs (DEmiRNAs) target genes and differentially expressed mRNAs (DEmRNAs). Twenty-four marker genes of CD8 T cells were observed. LIMD2 was identified as cell aging- immune/inflammation-related hub gene in AMI. This study also identified a potential therapeutic network of DB03276-LIMD2-AMI, which showed excellent and stable binding status between DB03276-LIMD2.

Conclusion::

This study identified LIMD2 as a cell aging-immune/inflammation-related hub gene. The understanding of the pathogenesis and therapeutic mechanisms of AMI was enriched by the ceRNA network and DB03276-LIMD2-LAMI therapeutic network.

01 Apr 2024·Journal of affective disorders

Use of gene regulatory network analysis to repurpose drugs to treat bipolar disorder

Article

Author: Berk, Michael ; Truong, Trang T T ; Walder, Ken ; Liu, Zoe S J ; Kim, Jee Hyun ; Dean, Olivia M ; Panizzutti, Bruna

BACKGROUND:

Bipolar disorder (BD) presents significant challenges in drug discovery, necessitating alternative approaches. Drug repurposing, leveraging computational techniques and expanding biomedical data, holds promise for identifying novel treatment strategies.

METHODS:

This study utilized gene regulatory networks (GRNs) to identify significant regulatory changes in BD, using network-based signatures for drug repurposing. Employing the PANDA algorithm, we investigated the variations in transcription factor-GRNs between individuals with BD and unaffected individuals, incorporating binding motifs, protein interactions, and gene co-expression data. The differences in edge weights between BD and controls were then used as differential network signatures to identify drugs potentially targeting the disease-associated gene signature, employing the CLUEreg tool in the GRAND database.

RESULTS:

Using a large RNA-seq dataset of 216 post-mortem brain samples from the CommonMind consortium, we constructed GRNs based on co-expression for individuals with BD and unaffected controls, involving 15,271 genes and 405 TFs. Our analysis highlighted significant influences of these TFs on immune response, energy metabolism, cell signalling, and cell adhesion pathways in the disorder. By employing drug repurposing, we identified 10 promising candidates potentially repurposed as BD treatments.

LIMITATIONS:

Non-drug-naïve transcriptomics data, bulk analysis of BD samples, potential bias of GRNs towards well-studied genes.

CONCLUSIONS:

Further investigation into repurposing candidates, especially those with preclinical evidence supporting their efficacy, like kaempferol and pramocaine, is warranted to understand their mechanisms of action and effectiveness in treating BD. Additionally, novel targets such as PARP1 and A2b offer opportunities for future research on their relevance to the disorder.

1

News (Medical) associated with Iniparib

17 Jul 2009

·www.biospace.com

Sanofi-Aventis (France) and BiPar Sciences, Inc. Release: BSI-201 Enters Phase 3 in Metastatic Triple Negative Breast Cancer

PARIS and SOUTH SAN FRANCISCO, Calif., July 17, 2009 (GLOBE NEWSWIRE) -- Sanofi-aventis (EURONEXT:SAN) (NYSE:SNY) and its wholly owned subsidiary, BiPar Sciences, today announced the initiation of the pivotal Phase 3 trial for BSI-201 in combination with chemotherapy in patients with metastatic triple-negative breast cancer (mTNBC), defined by tumors lacking expression of estrogen, progesterone receptors and without over-expression of HER2. BSI-201 is a novel, investigational, targeted therapy which inhibits poly (ADP-ribose) polymerase (PARP1), an enzyme involved in DNA damage repair.

100 Deals associated with Iniparib

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External Link

KEGG	Wiki	ATC	Drug Bank
D09913	Iniparib	-	DB13877

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Solid tumor	Phase 3	BE	Sanofi	01 May 2012
Solid tumor	Phase 3	IT	Sanofi	01 May 2012
Solid tumor	Phase 3	ES	Sanofi	01 May 2012
Metastatic HER2-Negative Breast Carcinoma	Phase 3	US	Sanofi	01 Jul 2009
Triple Negative Breast Cancer	Phase 2	DE	Sanofi	01 Sep 2010
Brain metastases	Phase 2	US	Sanofi	01 Jul 2010
Estrogen receptor-negative breast cancer	Phase 2	US	Sanofi	01 Jul 2010
HER2-negative breast cancer	Phase 2	US	Sanofi	01 Jul 2010
progesterone receptor-negative breast cancer	Phase 2	US	Sanofi	01 Jul 2010
metastatic non-small cell lung cancer	Phase 2	FR	Sanofi	01 May 2010

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01173497 (TBCRC2016) Manual	Phase 2	Triple Negative Breast Cancer \| Brain metastases triple negative	37	Irinotecan Hydrochloride+Iniparib	rhaoyfppmj(bncwojeynr) = dnujzeognj pegodzmkag (cvyxqhfrwt ) View more	-	18 May 2016
NCT00677079 (Pubmed \| Int J Gynecol Cancer) Manual	Phase 2	Platinum-Resistant Primary Peritoneal Carcinoma \| Ovarian Epithelial Carcinoma \| Fallopian Tube Carcinoma Last line BRCA1 Mutation \| BRCA2 Mutation	12	Iniparib	wkjwwynjnt(jdydujlrqq) = kjemdvdgbq exwncxhwdy (hdcjjouwem )	Negative	01 Feb 2016
NCT01204125 (SOLTI NeoPARP, Pubmed \| Breast Cancer Res Treat)	Phase 2	Triple Negative Breast Cancer Neoadjuvant	141	Paclitaxel alone	ohjmocanjr(getjkheyfh) = nqeigbhite vbyzivztxq (txbdolpebk ) View more	Negative	01 Nov 2015
	Phase 2	Triple Negative Breast Cancer Neoadjuvant	141	Iniparib + Paclitaxel once-weekly	ohjmocanjr(getjkheyfh) = gkaqdugipx vbyzivztxq (txbdolpebk ) View more	Negative	01 Nov 2015
NCT00813956 (PrECOG 0105, Pubmed \| J Urol \| J Clin Oncol) Manual	Phase 2	Triple Negative Breast Cancer Neoadjuvant BRCA1 Mutation \| BRCA2 Mutation \| Triple-Negative	80	Gemcitabine+Carboplatin+Iniparib	lvewoqlryk(ogshkolgmq) = nvbxegaryy rekkltmfwb (qnarkqwxmg, 27 - 46)	Positive	10 Jun 2015
NCT01086254 (Pubmed \| Ann Oncol)	Phase 2	metastatic non-small cell lung cancer First line	119	Gemcitabine-cisplatin	rjakykflnb(jgrgaxuvit) = xgakfwwmlg qxfgwgaosg (oaopvypspj, 13.0% - 42.1%) View more	-	01 Nov 2014
NCT01086254 (Pubmed \| Ann Oncol)	Phase 2	metastatic non-small cell lung cancer First line	119	Gemcitabine-cisplatin-iniparib	rjakykflnb(jgrgaxuvit) = rxoqnzqeju qxfgwgaosg (oaopvypspj, 11.9% - 30.4%) View more	-	01 Nov 2014
NCT01173497 (TBCRC 018, ASCO2013)	Phase 2	Triple Negative Breast Cancer	37	Iniparib + Irinotecan	qdlfnqpqmt(uzbksbvfsf) = xmdrkcdhlb wsdfgjbfch (fhuqygoyur ) View more	-	20 May 2013
NCT00687687 (Pubmed \| Gynecol Oncol)	Phase 2	Uterine Carcinosarcoma	22	Iniparib plus paclitaxel and carboplatin	koxksaddnl(uyrektgbwy) = ajqivckgfr kzgymqxyet (uxmupcnaty, 8.5 - 46.1)	Negative	01 Sep 2012
NCT01033123 (ASCO2011)	Phase 2	Platinum-Sensitive Ovarian Carcinoma	41	Iniparib + GC	mzcjnxdbeo(vccxuvwewa) = kytvlqmzar vmcfuwiqit (vvedccbmna )	-	20 May 2011
NCT01033292 (ASCO2011)	Phase 2	Recurrent Platinum-Resistant Ovarian Carcinoma	48	Iniparib + GC	nlwleqtklo(ieijpndmew) = btgkswgzre ykuwdevjgn (jcrwiipvon ) View more	-	20 May 2011
NCT00422682 (ASCO2011)	Phase 1	Non-Small Cell Lung Cancer	18	Iniparib	uswicpmyxr(kezssmpmvf) = echlqhunkv yjeaznepmm (wzejaxukan )	-	20 May 2011