Brepocitinib

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Brepocitinib
Brepocitinib.svg
Identifiers
  • [(1S)-2,2-difluorocyclopropyl]-[(1R,5S)-3-[2-[(1-methylpyrazol-4-yl)amino]pyrimidin-4-yl]-3,8-diazabicyclo[3.2.1]octan-8-yl]methanone
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
Formula C18H21F2N7O
Molar mass 389.411 g·mol−1
3D model (JSmol)
  • CN1C=C(C=N1)NC2=NC=CC(=N2)N3C[C@H]4CC[C@@H](C3)N4C(=O)[C@@H]5CC5(F)F
  • InChI=1S/C18H21F2N7O/c1-25-8-11(7-22-25)23-17-21-5-4-15(24-17)26-9-12-2-3-13(10-26)27(12)16(28)14-6-18(14,19)20/h4-5,7-8,12-14H,2-3,6,9-10H2,1H3,(H,21,23,24)/t12-,13+,14-/m0/s1
  • Key:BUWBRTXGQRBBHG-MJBXVCDLSA-N

Brepocitinib (PF-06700841) is a drug which acts as a dual inhibitor of JAK1 and TYK2, and was developed for the treatment of plaque psoriasis. [1] [2] [3] [4]

See also

Related Research Articles

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<span class="mw-page-title-main">Apremilast</span> Medication for psoriasis and psoriatic arthritis

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<span class="mw-page-title-main">Crisaborole</span> Chemical compound

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Calcipotriol/betamethasone dipropionate, sold under the brand name Taclonex among others, is a fixed-dose combination medication of the synthetic vitamin D3 analog calcipotriol (also known as calcipotriene) and the synthetic corticosteroid betamethasone dipropionate for the treatment of plaque psoriasis. It is used in the form of ointment, topical suspension, gel, aerosol, and foam.

<span class="mw-page-title-main">Janus kinase 3 inhibitor</span>

Janus kinase 3 inhibitors, also called JAK3 inhibitors, are a new class of immunomodulatory agents that inhibit Janus kinase 3. They are used for the treatment of autoimmune diseases. The Janus kinases are a family of four nonreceptor tyrosine-protein kinases, JAK1, JAK2, JAK3, and TYK2. They signal via the JAK/STAT pathway, which is important in regulating the immune system. Expression of JAK3 is largely restricted to lymphocytes, while the others are ubiquitously expressed, so selective targeting of JAK3 over the other JAK isozymes is attractive as a possible treatment of autoimmune diseases.

Bimekizumab, sold under the brand name Bimzelx, is a humanized anti-IL17A, anti-IL-17F, and anti-IL17AF monoclonal antibody that is used to treat plaque psoriasis, psoriatic arthritis, axial spondyloarthritis, and ankylosing spondylitis.

<span class="mw-page-title-main">Abrocitinib</span> Chemical compound

Abrocitinib, sold under the brand name Cibinqo, is a medication used for the treatment of atopic dermatitis (eczema). It is a Janus kinase inhibitor and it was developed by Pfizer. It is taken by mouth.

<span class="mw-page-title-main">Tapinarof</span> Chemical compound

Tapinarof, also known as benvitimod and sold under the brand name Vtama, is a medication used for the treatment of plaque psoriasis. The medication is applied to the skin. Besides its use in medicine, tapinarof is a naturally occurring compound found in bacterial symbionts of nematodes which has antibiotic properties.

<span class="mw-page-title-main">Deucravacitinib</span> Chemical compound

Deucravacitinib, sold under the brand name Sotyktu, is a medication used for the treatment of moderate-to-severe plaque psoriasis. It is a tyrosine kinase 2 (TYK2) inhibitor and it is taken by mouth. It was developed by Bristol Myers Squibb.

<span class="mw-page-title-main">Gusacitinib</span> Chemical compound

Gusacitinib (ASN002) is an investigational drug which acts as a pan-Janus kinase inhibitor, binding with similar affinity at JAK1, JAK2, JAK3 and TYK2, and also inhibiting spleen tyrosine kinase (SYK). It is taken orally and was developed for the treatment of eczema and dermatitis.

<span class="mw-page-title-main">Ropsacitinib</span> Chemical compound

Ropsacitinib (PF-06826647) is a drug which is an orally active, selective tyrosine kinase 2 (TYK2) inhibitor. It has been researched for various autoimmune inflammatory conditions, primarily plaque psoriasis.

References

  1. Fensome A, Ambler CM, Arnold E, Banker ME, Brown MF, Chrencik J, et al. (October 2018). "Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)". Journal of Medicinal Chemistry. 61 (19): 8597–8612. doi:10.1021/acs.jmedchem.8b00917. PMID   30113844.
  2. Forman SB, Pariser DM, Poulin Y, Vincent MS, Gilbert SA, Kieras EM, et al. (December 2020). "TYK2/JAK1 Inhibitor PF-06700841 in Patients with Plaque Psoriasis: Phase IIa, Randomized, Double-Blind, Placebo-Controlled Trial". The Journal of Investigative Dermatology. 140 (12): 2359–2370.e5. doi: 10.1016/j.jid.2020.03.962 . PMID   32311398.
  3. Martin G (February 2023). "Novel Therapies in Plaque Psoriasis: A Review of Tyrosine Kinase 2 Inhibitors". Dermatology and Therapy. 13 (2): 417–435. doi:10.1007/s13555-022-00878-9. PMC   9884727 . PMID   36592300.
  4. Caso F, Costa L, Triggianese P, Maione F, Bertolini N, Vastarella M, et al. (May 2023). "Recent developments for new investigational JAK inhibitors in psoriatic arthritis". Expert Opinion on Investigational Drugs. 32 (5): 361–371. doi:10.1080/13543784.2023.2207737. PMID   37096862.