Name | Ritlecitinib |
CAS number | 1792180-81-4 |
Description | Ritlecitinib is an orally administered, small molecule kinase inhibitor classified as a selective covalent modifier, with the CAS Registry Number 1792180-81-4. |
Structural formula |  |
Molecular Formula | C15H19N5O |
Molecular Weight | 285.34 g/mol |
Appearance | White powder |
Quality Standard | 99% |
Storage Condition | Cool dry place( away from the light) |
Shelf Life | >2 years if stored properly |
Sample package | Aluminium foil bag |
Commercial package | Aluminium Tin, Fiber drum |
Origin | China |
Ritlecitinib More Info
Ritlecitinib is an orally administered, small molecule kinase inhibitor classified as a selective covalent modifier, with the CAS Registry Number 1792180-81-4. Its molecular structure is engineered to target a specific kinase domain with high precision, incorporating a functional group that forms a permanent covalent bond with a cysteine residue located near the ATP-binding site of its target enzyme. This mechanism ensures sustained inhibition even after the drug has been cleared from the bloodstream, contributing to its prolonged pharmacological activity.
The primary mechanism of action for ritlecitinib is the potent and selective inhibition of Janus kinase 3 and members of the tyrosine kinase expressed in hepatocellular carcinoma family of kinases. By covalently binding to JAK3, it effectively blocks the signaling pathway of several cytokines that are dependent on the common gamma chain for their function, including interleukins 2, 4, 7, 9, 15, and 21. This targeted approach is designed to suppress the inflammatory immune response more selectively than broader JAK inhibitors, with the intention of preserving the function of other JAK-dependent pathways.
The main clinical application of ritlecitinib is in the treatment of autoimmune and inflammatory conditions, with a significant focus on alopecia areata. It has been investigated for its ability to promote significant hair regrowth in patients with moderate to severe forms of this autoimmune disorder that leads to hair loss. By dampening the immune attack on hair follicles, it addresses the underlying pathophysiology. Its therapeutic scope is also being explored in other T-cell mediated conditions such as vitiligo, rheumatoid arthritis, and inflammatory bowel diseases.
This pharmaceutical is formulated for oral administration, typically as a capsule or tablet taken once daily. The oral bioavailability and its covalent mechanism allow for consistent and sustained target coverage with a convenient dosing schedule. Clinical trials have evaluated various dosing strengths to establish an optimal balance between efficacy and safety, with treatment regimens often initiated at a higher loading dose before transitioning to a lower maintenance dose for long-term management.
The safety profile of ritlecitinib is characterized by the known risks associated with immunomodulation, though its selective target aims to mitigate some of the broader immunosuppressive effects. Common adverse events observed in clinical trials include headache, nasopharyngitis, and upper respiratory tract infections. As with many agents that suppress immune function, there is an increased susceptibility to infections, including herpes zoster, and a potential increased risk for malignancies. Regular laboratory monitoring for changes in lymphocyte counts, liver enzymes, and lipid levels is recommended during treatment to manage potential risks.
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