Drug intelligence / Profile preview

sangivamycin

Development stage
Discontinued
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous, Topical
01

Overview

Sangivamycin is a pyrrolo[2,3-d]pyrimidine nucleoside analog with broad-spectrum antiviral and antitumor activity. It functions primarily as an inhibitor of cellular kinases, notably **protein kinase C (PKC)** (Ki ≈ 10 μM) and **Haspin kinase**, impairing cellular processes like mitosis and cell cycle progression. In antiviral contexts, sangivamycin potently inhibits replication of RNA and DNA viruses, including arenaviruses, filoviruses, orthopoxviruses, and multiple SARS-CoV-2 variants at low nanomolar concentrations, showing greater efficacy than remdesivir in vitro. Its anti-cancer effects arise from the inhibition of kinases related to cell proliferation and survival, induction of cell cycle arrest, and promotion of apoptotic cell death. Sangivamycin has undergone historical clinical investigation in various malignancies and is tolerated with a favorable toxicity profile. Recent studies support continued preclinical and clinical development for **COVID-19** and potentially other viral diseases and cancers[1][3][5][7].

Other names
sangivamycinmorimycinAntibiotic BA-90912
02

Targets

PKC (Protein kinase C family)P-TEFb (Positive transcription elongation factor b)GSG2 (Germ cell associated 2, haspin)RdRp (Coronavirus RNA-dependent RNA polymerase)

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