Abrocitinib

Abrocitinib, sold under the brand name Cibinqo, is a medication used for the treatment of atopic dermatitis (eczema).[3][4] It is a Janus kinase inhibitor and it was developed by Pfizer.[3][4] It is taken by mouth.[3]

Abrocitinib
Clinical data
Trade namesCibinqo
Other namesPF-04965842
AHFS/Drugs.comMonograph
License data
Routes of
administration		By mouth
Drug classJanus kinase inhibitor
ATC code
Legal status
Legal status
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)
  • CCCS(=O)(=O)NC1CC(N(C)c2ncnc3[nH]ccc23)C1
  • 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+ checkY
  • Key:IUEWXNHSKRWHDY-PHIMTYICSA-N checkY

The most common side effects include nausea (feeling sick), headache, acne, herpes simplex (viral infection of the mouth or the genitals), increased levels of creatine phosphokinase in the blood (an enzyme released into the blood when muscle is damaged), vomiting, dizziness and pain in the upper belly.[4]

Abrocitinib was approved for medical use in the European Union in December 2021,[4] and in the United States in January 2022.[5]

Medical uses

In the EU, abrocitinib is indicated for the treatment of moderate-to-severe atopic dermatitis in adults who are candidates for systemic therapy.[4]

In the US, abrocitinib is indicated for the treatment of people twelve years of age and older with refractory, moderate-to-severe atopic dermatitis whose disease is not adequately controlled with other systemic drug products, including biologics, or when use of those therapies is inadvisable.[3]

Side effects

The most common adverse effects in studies were upper respiratory tract infection, headache, nausea, and diarrhea.[6]

Pharmacology

Mechanism of action

It is a selective inhibitor of the enzyme janus kinase 1 (JAK1).[6]

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.[7]

History
  • April 2016: initiation of Phase 2b trial
  • December 2017: initiation of JADE Mono-1 Phase 3 trial[8]
  • May 2018: Results of Phase 2b trial posted
  • October 2019: Results of Phase 3 trial presented[9]
  • June 2020: Results of second Phase 3 trial published[10]

Society and culture

In 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.[11] The applicant for this medicinal product is Pfizer Europe MA EEIG.[11] In December 2021, the European Commission approved abrocitinib for the treatment of atopic dermatitis.[4][12][13]

In January 2022, the US Food and Drug Administration (FDA) approved abrocitinib for adults with moderate-to-severe atopic dermatitis.[14]

References
  1. "Cibinqo Product information". Health Canada. 25 April 2012. Retrieved 30 September 2022.
  2. "Summary Basis of Decision - Cibinqo". Health Canada. 23 October 2014. Retrieved 23 February 2023.
  3. "Cibinqo- abrocitinib tablet, film coated". DailyMed. 15 February 2022. Retrieved 3 March 2022.
  4. "Cibinqo EPAR". European Medicines Agency (EMA). 11 October 2021. Retrieved 17 December 2021. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  5. "Drug Approval Package: Cibinqo". U.S. Food and Drug Administration (FDA). 10 February 2022. Retrieved 10 February 2023.
  6. 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.
  7. 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.
  8. 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
  9. "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.
  10. 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.
  11. "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.
  12. "European Commission Approves Pfizer's Cibinqo (abrocitinib) for the Treatment of Adults with Moderate-to-Severe Atopic Dermatitis". Pfizer Inc. (Press release). 10 December 2021. Retrieved 17 December 2021.
  13. "Cibinqo Product information". Union Register of medicinal products. Retrieved 3 March 2023.
  14. "U.S. FDA Approves Pfizer's Cibinqo (abrocitinib) for Adults with Moderate-to-Severe Atopic Dermatitis". Pfizer Inc. (Press release). 14 January 2022. Retrieved 16 January 2022.
  • "Abrocitinib". Drug Information Portal. U.S. National Library of Medicine.
  • 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
  • Clinical trial number NCT03575871 for "Study Evaluating Efficacy and Safety of PF-04965842 in Subjects Aged 12 Years And Older With Moderate to Severe Atopic Dermatitis (JADE Mono-2)" at ClinicalTrials.gov
  • Clinical trial number NCT03720470 for "Study Evaluating Efficacy and Safety of PF-04965842 and Dupilumab in Adult Subjects With Moderate to Severe Atopic Dermatitis on Background Topical Therapy (JADE Compare)" at ClinicalTrials.gov
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