Overview

NCI Definition [1]:
An orally bioavailable second mitochondrial-derived activator of caspases (SMAC) mimetic and inhibitor of IAP (Inhibitor of Apoptosis Protein) family of proteins, with potential antineoplastic activity. SMAC mimetic LCL161 binds to IAPs, such as X chromosome-linked IAP (XIAP) and cellular IAPs 1 and 2. Since IAPs shield cancer cells from the apoptosis process, this agent may restore and promote the induction of apoptosis through apoptotic signaling pathways in cancer cells. IAPs are overexpressed by many cancer cell types and suppress apoptosis by binding and inhibiting active caspases-3, -7 and -9, which play essential roles in apoptosis (programmed cell death), necrosis and inflammation.

Lcl161 has been investigated in 3 clinical trials, of which 2 are open and 1 is closed. Of the trials investigating lcl161, 2 are phase 1 (1 open) and 1 is phase 2 (1 open).

ER Negative, ER No Expression, and HER2 Deficient Expression are the most frequent biomarker inclusion criteria for lcl161 clinical trials.

Breast carcinoma, colorectal carcinoma, and multiple myeloma are the most common diseases being investigated in lcl161 clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Lcl161
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Lcl161
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating lcl161 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]:
smac mimetic lcl161
Drug Categories [2]:
IAP inhibitors
Drug Target(s) [2]:
BIRC2, BIRC3, BIRC5, BIRC7, XIAP
NCIT ID [1]:
C91079

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.