Zasocitinib

Zasocitinib
Identifiers
  • N-((1R,2R)-2-methoxycyclobutyl)-7-(methylamino)-5-{[2-oxo-1-(pyridin-2-yl)-1H-pyridin-3-yl]amino}pyrazolo[1,5-a]pyrimidine-3-carboxamide
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC23H24N8O3
Molar mass460.498 g·mol−1
3D model (JSmol)
  • CNc1cc(Nc2cccn(-c3ccccn3)c2=O)nc2c(C(=O)N[C@@H]3CC[C@H]3OC)cnn12
  • InChI=1S/C23H24N8O3/c1-24-20-12-18(27-16-6-5-11-30(23(16)33)19-7-3-4-10-25-19)29-21-14(13-26-31(20)21)22(32)28-15-8-9-17(15)34-2/h3-7,10-13,15,17,24H,8-9H2,1-2H3,(H,27,29)(H,28,32)/t15-,17-/m1/s1
  • Key:BWINBHTTZLVXGT-NVXWUHKLSA-N

Zasocitinib (TAK-279, NDI-034858) is a drug which is an orally active, highly selective, allosteric tyrosine kinase 2 (TYK2) inhibitor. It has been researched for various inflammatory conditions including psoriasis, psoriatic arthritis and Crohn's disease.[1][2][3] It is significantly more selective than earlier compounds over side targets such as JAK1, which is hoped to give it an improved side effect profile.[4] Phase 3 clinical trials for plaque psoriasis reported twice the effectiveness as the current best pill [5]

See also

References

  1. ^ Leit S, Greenwood J, Carriero S, Mondal S, Abel R, Ashwell M, et al. (August 2023). "Discovery of a Potent and Selective Tyrosine Kinase 2 Inhibitor: TAK-279". Journal of Medicinal Chemistry. 66 (15): 10473–10496. doi:10.1021/acs.jmedchem.3c00600. PMID 37427891.
  2. ^ Kivitz AJ (14 November 2023). "The investigational tyrosine kinase inhibitor TAK-279 is effective and well tolerated in patients with active psoriatic arthritis in phase 2b study". Cleveland Clinic Journal of Medicine.
  3. ^ Kivitz A, Muensterman ET, Kavanaugh A, Van der Heijde D, Klimiuk PA, Valenzuela G, et al. (24 October 2023). "Efficacy and Safety Outcomes of TAK-279, a Selective Oral Tyrosine Kinase 2 (TYK2) Inhibitor, from a Randomized, Double-blind, Placebo-controlled Phase 2b Trial in Patients with Active Psoriatic Arthritis". American College of Rheumatology.
  4. ^ "The Discovery Process of TAK-279 and the Deep Logic Behind its Acquisition by Takeda". synapse.patsnap.com. 10 August 2023.
  5. ^ "Takeda's Zasocitinib Delivered Rapid and Durable Skin Clearance in a Convenient Once-Daily Pill, Affirming Promise to Reshape Psoriasis Care". www.takeda.com. 28 March 2026.
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