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apg-1387

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Overview

NCI Definition [1]:
A small molecule, second mitochondria-derived activator of caspases (SMAC)-mimetic targeting inhibitor of apoptosis proteins (IAPs) with potential apoptosis-inducing and antineoplastic activities. Upon administration, IAP inhibitor APG-1387 selectively binds to and inhibits the activity of IAPs including X chromosome-linked IAP (XIAP) and cellular IAPs 1 (c-IAP1) and 2 (c-IAP2). This may restore and promote the induction of apoptosis through apoptotic signaling pathways and enhance proteasomal degradation of IAPs. Additionally, APG-1387 may work synergistically with cytotoxic drugs to overcome tumor cell resistance to apoptosis. IAPs are overexpressed by many cancer cell types, suppressing apoptosis by binding and inhibiting active caspases-3, -7 and -9 via their BIR (baculoviral lAP repeat) domains.

Clinical Trials

View Clinical Trials for apg-1387

Apg-1387 has been investigated in 2 clinical trials, of which 2 are open and 0 are closed. Of the trials investigating apg-1387, 1 is phase 1 (1 open) and 1 is phase 1/phase 2 (1 open).

Microsatellite Stable (MSS) is the most frequent biomarker inclusion criterion for apg-1387 clinical trials.

Malignant solid tumor, colorectal carcinoma, and hematopoietic and lymphoid malignancy are the most common diseases being investigated in apg-1387 clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Apg-1387
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating apg-1387 and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
apg1387, apg 1387, smac-mimetic apg-1387, sm-1387, pyrrolo(1,2-a)(1,5)diazocine-8-carboxamide, 3,3'-(1,3-phenylenebis(sulfonyl))bis(n-(diphenylmethyl)decahydro-5-(((2s)-2-(methylamino)-1-oxopropyl)amino)-6-oxo-, (5s,5's,8s,8's,10ar,10'ar)-, iap inhibitor apg-1387, iap antagonist apg-1387
Drug Target(s) [2]:
BIRC2, BIRC3, XIAP
NCIT ID [1]:
C162535

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.