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

General Information of Drug (ID: DMW3TGI)

• Drug Name: PCI-45292 Drug Info
• Synonyms: Btk inhibitors (autoimmune disease); Btk inhibitors (autoimmune disease), Pharmacyclics; Bruton's tyrosine kinase inhibitors (autoimmune disease), Pharmacyclics

Indication

Disease Entry	ICD 11	Status	REF
Autoimmune diabetes	5A10	Preclinical	[1]

• Cross-matching ID: TTD Drug ID: DMW3TGI

Molecule-Related Drug Atlas

Drug(s) Targeting Tyrosine-protein kinase BTK (ATK)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ibrutinib	DMHZCPO	Mantle cell lymphoma	2A85.5	Approved	[3]
Acalabrutinib	DM7GCVW	leukaemia	2A60-2B33	Approved	[4]
Zanubrutinib	DMJWRQP	Mantle cell lymphoma	2A85.5	Approved	[5]
Pirtobrutinib	DMRG1X3	Non-hodgkin lymphoma	2B33.5	Approved	[6]
GDC-0853	DMBEL3Q	Multiple sclerosis	8A40	Phase 3	[7]
ICP-022	DMU72KL	Chronic lymphocytic leukaemia	2A82.0	Phase 3	[8]
Tolebrutinib	DML19V6	Multiple sclerosis	8A40	Phase 3	[9]
CC-292	DMJR9H0	Chronic lymphocytic leukaemia	2A82.0	Phase 2	[10]
BMS-986142	DMZB8AJ	Rheumatoid arthritis	FA20	Phase 2	[7]
LOU064	DME8O5K	Chronic idiopathic urticaria	EB00.1	Phase 2	[11]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Tyrosine-protein kinase BTK (ATK)	TTGM6VW	BTK_HUMAN	Inhibitor	[2]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029717)
• [2] Ibrutinib is an irreversible molecular inhibitor of ITK driving a Th1-selective pressure in T lymphocytes. Blood. 2013 October 10; 122(15): 2539-2549.
• [3] 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: 1948).
• [4] 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [6] Targeting BTK in CLL: Beyond Ibrutinib. Curr Hematol Malig Rep. 2019 Jun;14(3):197-205.
• [7] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [8] Clinical pipeline report, company report or official report of InnoCare Pharma.
• [9] Safety and efficacy of tolebrutinib, an oral brain-penetrant BTK inhibitor, in relapsing multiple sclerosis: a phase 2b, randomised, double-blind, placebo-controlled trial. Lancet Neurol. 2021 Sep;20(9):729-738.
• [10] Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans. J Pharmacol Exp Ther. 2013 Aug;346(2):219-28.
• [11] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)