Abrocitinib

Abrocitinib
Clinical data
Other names	PF-04965842
Routes of; administration	By mouth
Pharmacokinetic data
Elimination half-life	2.8–5.2 h
Excretion	1.0–4.4% unchanged in urine
Identifiers
CAS Number	1622902-68-4;
PubChem CID	78323835;
DrugBank	DB14973 ;
ChemSpider	68006894 ;
UNII	73SM5SF3OR;
KEGG	D11400 ;
ChEMBL	ChEMBL3655081;
ECHA InfoCard	100.251.498
Chemical and physical data
Formula	C14H21N5O2S
Molar mass	323.42 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CCCS(=O)(=O)NC1CC(C1)N(C)C2=NC=NC3=C2C=CN3;
	InChI 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+ ; Key:IUEWXNHSKRWHDY-PHIMTYICSA-N ;

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.

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]

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References

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.
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.
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
"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.
"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)

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[Gooderham-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)