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silmitasertib
- Development stage
- Phase 2
- Lead developer
- Senhwa Biosciences
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Silmitasertib (CX-4945) is an orally bioavailable, small-molecule inhibitor of casein kinase 2 (CK2), a serine/threonine-specific protein kinase that is constitutively active and overexpressed in several types of tumors. It acts as an ATP-competitive inhibitor targeting both CK2α and CK2α′ catalytic subunits. Silmitasertib also inhibits other kinases, including DYRK1A and GSK3β, with demonstrated activity in limiting their downstream signaling pathways[1][2][3][7]. The drug has shown anti-proliferative effects in various cancer cell lines by suppressing the PI3K/Akt/mTOR pathway, inducing apoptosis, causing cell cycle arrest, and repressing BCL-XL expression[1][6]. Silmitasertib is being developed primarily for oncology indications such as cholangiocarcinoma (bile duct cancer), recurrent Sonic Hedgehog medulloblastoma, acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL), and other hematological malignancies[1][6][7]. It was granted orphan drug status by the FDA for advanced cholangiocarcinoma. The developer is Senhwa Biosciences.
- Other names
- silmitasertib
02
Targets
CK2 (Casein kinase II subunit alpha)CSNK2A2 (Casein kinase II subunit alpha prime)DYRK1A (Dual-specificity tyrosine-phosphorylation-regulated kinase 1A)GSK3 (Glycogen synthase kinase 3 beta)
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