Drugs /

tolinapant

Back to Drugs List

Overview

NCI Definition [1]:
An orally bioavailable, non-peptidomimetic antagonist of both X chromosome-linked inhibitor of apoptosis protein (XIAP) and cellular IAP 1 (cIAP1), with potential antineoplastic and pro-apoptotic activities. Upon administration, tolinapant selectively binds to and inhibits the activity of XIAP and cIAP1. This restores and promotes the induction of apoptotic signaling pathways in cancer cells, and inactivates the nuclear factor-kappa B (NF-kB)-mediated survival pathway. XIAP and cIAP1 are overexpressed by many cancer cell types and suppress apoptosis by inhibiting the activity of certain caspases; they promote both cancer cell survival and chemotherapy resistance.

Clinical Trials

View Clinical Trials for tolinapant

Tolinapant has been investigated in 3 clinical trials, of which 3 are open and 0 are closed. Of the trials investigating tolinapant, 1 is phase 1 (1 open) and 2 are phase 1/phase 2 (2 open).

BCR-ABL1 Fusion, BIRC2 Amplification, and BIRC3 Amplification are the most frequent biomarker inclusion criteria for tolinapant clinical trials.

Acute myeloid leukemia, adult T-cell acute lymphoblastic leukemia, and anaplastic large cell lymphoma are the most common diseases being investigated in tolinapant clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Tolinapant
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating tolinapant 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]:
astx660, astx 660, xiap/ciap1 antagonist astx660
Drug Target(s) [2]:
BIRC2, XIAP
NCIT ID [1]:
C123913

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.