abrocitinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
Janus kinase inhibitors, antineoplastics 5504 1622902-68-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • abrocitinib
  • cibinqo
  • PF-04965842
Abrocitinib is a Janus kinase (JAK)1 inhibitor. JAKs phosphorylate and activate Signal Transducers and Activators of Transcription (STATs) which modulate intracellular activity including gene expression. Inhibition of JAK1 modulates the signalling pathways by preventing the phosphorylation and activation of STATs. It is used for treating adults with moderate to severe atopic dermatitis (also known as eczema, when the skin is itchy, red and dry).
  • Molecular weight: 323.42
  • Formula: C14H21N5O2S
  • CLOGP: 2.54
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 90.98
  • ALOGS: -2.89
  • ROTB: 5
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.15 g O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Dec. 9, 2021 EMA PFIZER EUROPE MA EEIG
Jan. 14, 2022 FDA PFIZER Inc
Sept. 27, 2021 PMDA PFIZER JAPAN INC.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Eczema herpeticum 57.41 55.89 7 262 162 63488591

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Therapeutic product effect incomplete 79.20 46.19 31 498 141614 79602245
Eczema herpeticum 75.06 46.19 10 519 298 79743561
Condition aggravated 49.29 46.19 34 495 501090 79242769

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC D11AH08 DERMATOLOGICALS
OTHER DERMATOLOGICAL PREPARATIONS
OTHER DERMATOLOGICAL PREPARATIONS
Agents for dermatitis, excluding corticosteroids
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000190857 Janus Kinase Inhibitors
FDA EPC N0000190858 Janus Kinase Inhibitor

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Atopic dermatitis indication 24079001 DOID:3310




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
100MG CIBINQO PFIZER N213871 Jan. 14, 2022 RX TABLET ORAL 9549929 Feb. 19, 2034 TREATMENT OF ADULTS WITH REFRACTORY, MODERATE-TO-SEVERE ATOPIC DERMATITIS NOT ADEQUATELY CONTROLLED WITH OTHER SYSTEMIC DRUG PRODUCTS OR WHEN USE OF THOSE THERAPIES IS INADVISABLE
200MG CIBINQO PFIZER N213871 Jan. 14, 2022 RX TABLET ORAL 9549929 Feb. 19, 2034 TREATMENT OF ADULTS WITH REFRACTORY, MODERATE-TO-SEVERE ATOPIC DERMATITIS NOT ADEQUATELY CONTROLLED WITH OTHER SYSTEMIC DRUG PRODUCTS OR WHEN USE OF THOSE THERAPIES IS INADVISABLE
50MG CIBINQO PFIZER N213871 Jan. 14, 2022 RX TABLET ORAL 9549929 Feb. 19, 2034 TREATMENT OF ADULTS WITH REFRACTORY, MODERATE-TO-SEVERE ATOPIC DERMATITIS NOT ADEQUATELY CONTROLLED WITH OTHER SYSTEMIC DRUG PRODUCTS OR WHEN USE OF THOSE THERAPIES IS INADVISABLE

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
100MG CIBINQO PFIZER N213871 Jan. 14, 2022 RX TABLET ORAL Feb. 9, 2026 NEW PATIENT POPULATION
200MG CIBINQO PFIZER N213871 Jan. 14, 2022 RX TABLET ORAL Feb. 9, 2026 NEW PATIENT POPULATION
50MG CIBINQO PFIZER N213871 Jan. 14, 2022 RX TABLET ORAL Feb. 9, 2026 NEW PATIENT POPULATION
100MG CIBINQO PFIZER N213871 Jan. 14, 2022 RX TABLET ORAL Jan. 14, 2027 NEW CHEMICAL ENTITY
200MG CIBINQO PFIZER N213871 Jan. 14, 2022 RX TABLET ORAL Jan. 14, 2027 NEW CHEMICAL ENTITY
50MG CIBINQO PFIZER N213871 Jan. 14, 2022 RX TABLET ORAL Jan. 14, 2027 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Tyrosine-protein kinase JAK1 Kinase INHIBITOR IC50 7.54 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Tyrosine-protein kinase JAK3 Kinase IC50 6.32 CHEMBL
Amine oxidase [flavin-containing] A Enzyme IC50 5.22 CHEMBL
Vascular endothelial growth factor receptor 2 Kinase IC50 5.92 CHEMBL
Non-receptor tyrosine-protein kinase TYK2 Kinase IC50 6.80 CHEMBL
Tyrosine-protein kinase JAK2 Kinase INHIBITOR IC50 6.10 SCIENTIFIC LITERATURE

External reference:

IDSource
CHEMBL3655081 ChEMBL_ID
C000634427 MESH_SUPPLEMENTAL_RECORD_UI
9991 IUPHAR_LIGAND_ID
DB14973 DRUGBANK_ID
018933 NDDF
4041157 VANDF
D11400 KEGG_DRUG
C5139788 UMLSCUI
11012 INN_ID
78323835 PUBCHEM_CID
2591476 RXNORM
353076 MMSL
40053 MMSL
d09824 MMSL
73SM5SF3OR UNII

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Cibinqo HUMAN PRESCRIPTION DRUG LABEL 1 0069-0235 TABLET, FILM COATED 50 mg ORAL NDA 34 sections
Cibinqo HUMAN PRESCRIPTION DRUG LABEL 1 0069-0235 TABLET, FILM COATED 50 mg ORAL NDA 34 sections
Cibinqo HUMAN PRESCRIPTION DRUG LABEL 1 0069-0335 TABLET, FILM COATED 100 mg ORAL NDA 34 sections
Cibinqo HUMAN PRESCRIPTION DRUG LABEL 1 0069-0335 TABLET, FILM COATED 100 mg ORAL NDA 34 sections
Cibinqo HUMAN PRESCRIPTION DRUG LABEL 1 0069-0435 TABLET, FILM COATED 200 mg ORAL NDA 34 sections
Cibinqo HUMAN PRESCRIPTION DRUG LABEL 1 0069-0435 TABLET, FILM COATED 200 mg ORAL NDA 34 sections
CIBINQO HUMAN PRESCRIPTION DRUG LABEL 1 63539-236 TABLET, FILM COATED 50 mg ORAL NDA 33 sections
CIBINQO HUMAN PRESCRIPTION DRUG LABEL 1 63539-336 TABLET, FILM COATED 100 mg ORAL NDA 33 sections
CIBINQO HUMAN PRESCRIPTION DRUG LABEL 1 63539-436 TABLET, FILM COATED 200 mg ORAL NDA 33 sections