Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMCNSII)

• Drug Name: GDC-0214 Drug Info
• Synonyms: GDC-0214; 1831144-46-7; iJak-381; N-(3-(5-Chloro-2-(difluoromethoxy)phenyl)-1-(2-(4-((2-cyanoethyl)(methyl)amino)piperidin-1-yl)-2-oxoethyl)-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide; Pyrazolo[1,5-a]pyrimidine-3-carboxylic acid [3-(5-chloro-2-difluoromethoxy-phenyl)-1-(2-{4-[(2-cyano-ethyl)-methyl-amino]-piperidin-1-yl}-2-oxo-ethyl)-1H-pyrazol-4-yl]-amide; N-[3-[5-chloro-2-(difluoromethoxy)phenyl]-1-[2-[4-[2-cyanoethyl(methyl)amino]piperidin-1-yl]-2-oxoethyl]pyrazol-4-yl]pyrazolo[1,5-a]pyrimidine-3-carboxamide; CHEMBL3964801; SCHEMBL17271636; GTPL12318; GDC0214; BDBM232517; EX-A6434; RG6151; AKOS040759985; RG-6151; US9346815, 63

Indication

Disease Entry	ICD 11	Status	REF
Asthma	CA23	Phase 1	[1]

• Cross-matching ID:
  PubChem CID: 118522534
  TTD Drug ID: DMCNSII

Molecule-Related Drug Atlas

Drug(s) Targeting Janus kinase 2 (JAK-2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Momelotinib	DMF98Q0	Myelofibrosis	2A20.2	Approved	[3]
Baricitinib	DM4ONW5	Rheumatoid arthritis	FA20	Approved	[4]
Ruxolitinib	DM7Q98D	Essential thrombocythemia	3B63.1Z	Approved	[5]
Pacritinib	DM1T6ZN	Myelofibrosis	2A20.2	Approved	[6]
Fedratinib	DM4ZBK6	Myelofibrosis	2A20.2	Approved	[7]
ITF2357	DMFZBNE	Duchenne dystrophy	8C70	Phase 3	[8]
XL019	DMJ6F5C	Solid tumour/cancer	2A00-2F9Z	Phase 3	[8]
Cerdulatinib	DMSCR2H	B-cell lymphoma	2A86	Phase 2	[9]
CTP-543	DM3SYOK	Alopecia	ED70	Phase 2	[10]
INCB039110	DMD9RV3	Malignant neoplasm	2A00-2F9Z	Phase 2	[11]

Drug(s) Targeting Janus kinase 1 (JAK-1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Baricitinib	DM4ONW5	Rheumatoid arthritis	FA20	Approved	[4]
Ruxolitinib	DM7Q98D	Essential thrombocythemia	3B63.1Z	Approved	[5]
Upadacitinib	DM32B5U	Rheumatoid arthritis	FA20	Approved	[12]
ASP-015K	DMZ1UOI	Psoriasis vulgaris	EA90	Phase 3	[13]
SHR0302	DMUL8ZT	Ulcerative colitis	DD71	Phase 3	[14]
Cerdulatinib	DMSCR2H	B-cell lymphoma	2A86	Phase 2	[15]
CTP-543	DM3SYOK	Alopecia	ED70	Phase 2	[10]
INCB039110	DMD9RV3	Malignant neoplasm	2A00-2F9Z	Phase 2	[13]
PF-06700841	DMMGSFV	Asthma	CA23	Phase 2	[15]
ATI-501	DMTY6OF	Alopecia	ED70	Phase 2	[16]

Drug(s) Targeting Janus kinase 3 (JAK-3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tofacitinib	DMBS370	Rheumatoid arthritis	FA20	Approved	[17]
Ritlecitinib	DMYKNME	Alopecia areata	ED70.2	Approved	[15]
ASP-015K	DMZ1UOI	Psoriasis vulgaris	EA90	Phase 3	[18]
VX-509	DM2U3MX	Rheumatoid arthritis	FA20	Phase 2/3	[4]
Cerdulatinib	DMSCR2H	B-cell lymphoma	2A86	Phase 2	[15]
ATI-501	DMTY6OF	Alopecia	ED70	Phase 2	[16]
ATI-502	DM8NODR	Alopecia	ED70	Phase 2	[19]
TD-8236	DMTOMJN	Asthma	CA23	Phase 2	[20]
ALXN2075	DM1BSD8	Non-hodgkin lymphoma	2B33.5	Phase 1/2	[21]
SNA-125	DM8L1GJ	Atopic dermatitis	EA80	Phase 1	[15]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Janus kinase 1 (JAK-1)	TT6DM01	JAK1_HUMAN	Inhibitor	[2]
Janus kinase 2 (JAK-2)	TTRMX3V	JAK2_HUMAN	Inhibitor	[2]
Janus kinase 3 (JAK-3)	TTT7PJU	JAK3_HUMAN	Inhibitor	[2]

References

• [1] Inhaled JAK inhibitor GDC-0214 reduces exhaled nitric oxide in patients with mild asthma: A?randomized, controlled, proof-of-activity trial. J Allergy Clin Immunol. 2021 Sep;148(3):783-789.
• [2] Inhaled JAK inhibitor GDC-0214 reduces exhaled nitric oxide in patients with mild asthma: A?randomized, controlled, proof-of-activity trial. J Allergy Clin Immunol. 2021 Sep;148(3):783-789.
• [3] Genetic determinants of response and survival in momelotinib-treated patients with myelofibrosis.Leukemia.2015 Mar;29(3):741-4.
• [4] Selective JAK inhibitors in development for rheumatoid arthritis. Expert Opin Investig Drugs. 2014 Aug;23(8):1067-77.
• [5] 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
• [6] National Cancer Institute Drug Dictionary (drug id 609888).
• [7] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [8] Emerging drugs for the therapy of primary and post essential thrombocythemia, post polycythemia vera myelofibrosis. Expert Opin Emerg Drugs. 2009 Sep;14(3):471-9.
• [9] Company report (Portola Pharmaceuticals)
• [10] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [11] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2048).
• [12] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [13] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2047).
• [14] Efficacy and Safety of SHR0302, a Highly Selective Janus Kinase 1 Inhibitor, in Patients with Moderate to Severe Atopic Dermatitis: A Phase II Randomized Clinical Trial. Am J Clin Dermatol. 2021 Nov;22(6):877-889.
• [15] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [16] Clinical pipeline report, company report or official report of Aclaris Therapeutics.
• [17] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [18] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2049).
• [19] ClinicalTrials.gov (NCT03759340) ATI-502 Topical Solution for the Treatment of Alopecia Areata (AA), Alopecia Universalis (AU) and Alopecia Totalis (AT). U.S. National Institutes of Health.
• [20] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight
• [21] The Dual Syk/JAK Inhibitor Cerdulatinib Antagonizes B-cell Receptor and Microenvironmental Signaling in Chronic Lymphocytic Leukemia. Clin Cancer Res. 2017 May 1;23(9):2313-2324.