Drug intelligence / Profile preview

TG100-115

Development stage
Phase 2
Lead developer
Sanofi
Modality
Small Molecules
Administration
Oral
01

Overview

TG100‑115 is a small molecule investigational drug that acts as a selective inhibitor of phosphatidylinositol 3‑kinase gamma (PI3Kγ) and delta (PI3Kδ). It has demonstrated potent inhibition of these PI3K isoforms with little effect on the alpha and beta isoforms. In preclinical studies, it has shown anti-inflammatory effects by reducing edema and inflammation in models relevant to myocardial infarction. Additionally, it inhibits the kinase activity of transient receptor potential melastatin 7 (TRPM7), which is implicated in cancer cell migration and invasion. The compound has been studied for its potential use in oncology (including breast cancer and glioblastoma), cardiovascular diseases such as ST elevation myocardial infarction, asthma, chronic obstructive pulmonary disease (COPD), and liver cancer[1][2][5][6].

Other names
3-(2,4-diamino-6-(3-hydroxyphenyl)pteridin-7-yl)phenol6,7-bis(3-hydroxyphenyl)pteridine-2,4-diamineUNII-7ACH1U1E2MUNII7ACH1U1E2MUNII 7ACH1U1E2MCAS 677297–51–7
02

Targets

Transient receptor potential cation channel subfamily M member 7 (TRPM7) kinase domainPIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CD (Phosphatidylinositol 3-kinase delta)

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