Drug intelligence / Profile preview

FIT-039

Development stage
Unknown
Lead developer
KinoPharma
Modality
Small Molecules
Administration
Topical, Transdermal, Transvaginal, Oral, Intravenous, Intraperitoneal
01

Overview

**FIT-039** is a selective small molecule inhibitor of cyclin-dependent kinase 9 (CDK9), developed by researchers at Kyoto University. It binds competitively to the ATP-binding pocket of CDK9/cyclin T1 (IC50 5.8 μM), suppressing transcriptional elongation by inhibiting phosphorylation of the RNA polymerase II C-terminal domain, thereby preventing replication of multiple DNA viruses including HSV-1 (including acyclovir-resistant strains), HCMV, HAdV, HPV, KSHV, and HBV. Unlike broader CDK inhibitors like flavopiridol, FIT-039 exhibits minimal cytotoxicity, limited impact on host cell transcriptome and cell cycle, and good tolerability in preclinical rodent models (up to 1000 mg/kg oral daily) and early clinical trials. It has advanced to phase I/II trials for topical/transdermal treatment of common warts (verruca vulgaris caused by HPV) and transvaginal tablets for cervical intraepithelial neoplasia (CIN1/2), showing safety with mild, self-limiting adverse events like vaginal discharge.[1][2][3][5][7]

Other names
CIN Vaginal TabletKinoPharma CIN treatment
02

Targets

GSG2 (Germ cell associated 2, haspin)RPS6KB1 (Ribosomal protein S6 kinase beta-1)CDK9 (Cyclin-dependent kinase 9)GSK3 (Glycogen synthase kinase 3 beta)DYRK1B (Dual specificity tyrosine-phosphorylation-regulated kinase 1B)DYRK3 (Dual-specificity tyrosine-phosphorylation-regulated kinase 3)INSRR (Insulin receptor-related receptor)PAK1 (p21-activated kinase 1)

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