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SGI-1776
- Development stage
- Discontinued
- Lead developer
- SuperGen
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
SGI-1776 is a small molecule, orally administered pan-PIM kinase inhibitor developed for the treatment of various cancers. It selectively inhibits the serine/threonine kinases PIM1, PIM2, and PIM3, which are implicated in cell cycle progression and inhibition of apoptosis. By blocking these kinases, SGI‑1776 disrupts G1/S phase cell cycle transition and promotes tumor cell apoptosis through increased expression of pro-apoptotic proteins such as Bcl2. Preclinical studies demonstrated antitumor activity in models of acute myeloid leukemia (AML), prostate cancer, and non-Hodgkin's lymphoma. Clinical trials were initiated for relapsed/refractory leukemias, prostate cancer, and non-Hodgkin's lymphoma; however, development was terminated due to dose-limiting cardiac toxicity (QTc prolongation)[1][2][3][8].
- Brand names
- SGI-1776SGI1776SGI 1776
- Other names
- UNII-72AUA0603WUNII72AUA0603WUNII 72AUA0603WCAS 1025065-69-3CAS1025065-69-3CAS-1025065-69-3
02
Targets
PIM3 (Proviral integration site for Moloney murine leukemia virus kinase 3)PIM1 (Proviral integration site for moloney murine leukemia virus kinase 1)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PIM2 (Proto-oncogene serine/threonine-protein kinase Pim2)FLT3 (Fms related receptor tyrosine kinase 3)GSG2 (Germ cell associated 2, haspin)
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