Abrocitinib

Abrocitinib (code name PF-04965842) is a Janus kinase inhibitor drug which is currently under investigation for the treatment of atopic dermatitis. It was developed by Pfizer.

Abrocitinib
Clinical data
Other namesPF-04965842
Routes of
administration		By mouth
Pharmacokinetic data
Elimination half-life2.8–5.2 h
Excretion1.0–4.4% unchanged in urine
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
ECHA InfoCard100.251.498
Chemical and physical data
FormulaC14H21N5O2S
Molar mass323.42 g·mol−1
3D model (JSmol)

Side effects

The most common adverse effects in studies were upper respiratory tract infection, headache, nausea, and diarrhea.[1]

Pharmacology

Mechanism of action

It is a selective inhibitor of the enzyme janus kinase 1 (JAK1).[1]

Pharmacokinetics

Abrocitinib is quickly absorbed from the gut and generally reaches highest blood plasma concentrations within one hour. Only 1.0 to 4.4% of the dose are found unmetabolized in the urine.[2]

Timeline
  • April 2016: initiation of Phase 2b trial
  • December 2017: initiation of JADE Mono-1 Phase 3 trial[3]
  • May 2018: Results of Phase 2b trial posted
  • October 2019: Results of Phase 3 trial presented[4]
  • June 2020: Results of second Phase 3 trial published[5]

References
  1. Gooderham MJ, Forman SB, Bissonnette R, Beebe JS, Zhang W, Banfield C, et al. (October 2019). "Efficacy and Safety of Oral Janus Kinase 1 Inhibitor Abrocitinib for Patients With Atopic Dermatitis: A Phase 2 Randomized Clinical Trial". JAMA Dermatology. doi:10.1001/jamadermatol.2019.2855. PMC 6777226. PMID 31577341.
  2. Peeva E, Hodge MR, Kieras E, Vazquez ML, Goteti K, Tarabar SG, et al. (August 2018). "Evaluation of a Janus kinase 1 inhibitor, PF-04965842, in healthy subjects: A phase 1, randomized, placebo-controlled, dose-escalation study". British Journal of Clinical Pharmacology. 84 (8): 1776–1788. doi:10.1111/bcp.13612. PMC 6046510. PMID 29672897.
  3. Clinical trial number NCT03349060 for "Study to Evaluate Efficacy and Safety of PF-04965842 in Subjects Aged 12 Years And Older With Moderate to Severe Atopic Dermatitis (JADE Mono-1)" at ClinicalTrials.gov
  4. "Pfizer Presents Positive Phase 3 Data at the 28th Congress of the European Academy of Dermatology and Venereology for Abrocitinib in Moderate to Severe Atopic Dermatitis". Drugs.com. 2019-10-12.
  5. "Efficacy and Safety of Abrocitinib in Patients With Moderate-to-Severe Atopic Dermatitis: A Randomized Clinical Trial". JAMA Dermatology. June 3, 2020. doi:10.1001/jamadermatol.2020.1406. Retrieved June 4, 2020. Cite journal requires |journal= (help)
This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.