Abrocitinib

Abrocitinib is a Janus kinase inhibitor medication which is under investigation for the treatment of atopic dermatitis. It was developed by Pfizer.

Abrocitinib
Clinical data
Other namesPF-04965842
Routes of
administration		By mouth
ATC code
  • None
Pharmacokinetic data
Elimination half-life2.8–5.2 h
Excretion1.0–4.4% unchanged in urine
Identifiers
CAS Number
  • 1622902-68-4
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)
  • CCCS(=O)(=O)NC1CC(C1)N(C)C2=NC=NC3=C2C=CN3
  • InChI=1S/C14H21N5O2S/c1-3-6-22(20,21)18-10-7-11(8-10)19(2)14-12-4-5-15-13(12)16-9-17-14/h4-5,9-11,18H,3,6-8H2,1-2H3,(H,15,16,17)/t10-,11+ Y
  • Key:IUEWXNHSKRWHDY-PHIMTYICSA-N Y

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]

Society and culture

On 14 October 2021, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Cibinqo, intended for the treatment of atopic dermatitis.[6] The applicant for this medicinal product is Pfizer Europe MA EEIG.[6]

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. 155 (12): 1371–1379. 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. 12 October 2019.
  5. Silverberg, J. I.; Simpson, E. L.; Thyssen, J. P.; Gooderham, M.; Chan, G.; Feeney, C.; Biswas, P.; Valdez, H.; Dibonaventura, M.; Nduaka, C.; Rojo, R. (3 June 2020). "Efficacy and Safety of Abrocitinib in Patients With Moderate-to-Severe Atopic Dermatitis: A Randomized Clinical Trial". JAMA Dermatology. 156 (8): 863–873. doi:10.1001/jamadermatol.2020.1406. PMC 7271424. PMID 32492087.
  6. "Cibinqo: Pending EC decision". European Medicines Agency. 15 October 2021. Retrieved 15 October 2021. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  • "Abrocitinib". Drug Information Portal. U.S. National Library of Medicine.


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