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

General Information of Drug (ID: DMFOXGB)

• Drug Name: INCB81776 Drug Info
• Synonyms: INCB081776

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Phase 1	[1]

• Cross-matching ID: TTD Drug ID: DMFOXGB

Molecule-Related Drug Atlas

Drug(s) Targeting Tyrosine-protein kinase Mer (MERTK)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[3]
ONO-7475	DMV6GX7	Acute leukaemia	2A60	Phase 1/2	[4]
ONO-7475	DMV6GX7	Acute leukaemia	2A60	Phase 1/2	[5]
RXDX-106	DM6NVTR	Solid tumour/cancer	2A00-2F9Z	Phase 1	[6]
MRX-2843	DMM5N8P	Solid tumour/cancer	2A00-2F9Z	Phase 1	[7]
PF-07265807	DMSMNRQ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[8]
LDC1267	DMH7R6L	Discovery agent	N.A.	Investigative	[9]
G749	DMC7HIS	Discovery agent	N.A.	Investigative	[10]
UNC2025	DMCU59W	Glioblastoma of brain	2A00.00	Investigative	[11]
UNC569	DMJL6ZM	Acute lymphoblastic leukaemia	2A85	Investigative	[12]

Drug(s) Targeting Tyrosine-protein kinase UFO (AXL)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Gilteritinib	DMTI0ZO	Acute myeloid leukaemia	2A60	Approved	[4]
MGCD265	DMRPCF2	Non-small-cell lung cancer	2C25.Y	Phase 2	[13]
BI-505	DMSZQHX	Multiple myeloma	2A83	Phase 2	[14]
Bemcentinib	DM0YCPL	Myelodysplastic syndrome	2A37	Phase 2	[15]
BGB-324	DMDI43Y	Breast cancer	2C60-2C65	Phase 2	[16]
Mecbotamab vedotin	DMU5KH4	Ovarian cancer	2C73	Phase 2	[17]
ONO-7475	DMV6GX7	Acute leukaemia	2A60	Phase 1/2	[4]
ONO-7475	DMV6GX7	Acute leukaemia	2A60	Phase 1/2	[5]
TP-0903	DMHTG8P	Chronic lymphocytic leukaemia	2A82.0	Phase 1/2	[4]
Enapotamab vedotin	DM1PQJO	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[18]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Tyrosine-protein kinase Mer (MERTK)	TTO7LKR	MERTK_HUMAN	Inhibitor	[2]
Tyrosine-protein kinase UFO (AXL)	TTZPY6J	UFO_HUMAN	Inhibitor	[2]

References

• [1] ClinicalTrials.gov (NCT03522142) A Study Exploring the Safety and Tolerability of INCB081776 in Participants With Advanced Malignancies. U.S. National Institutes of Health.
• [2] A Potent and Selective Dual Inhibitor of AXL and MERTK Possesses Both Immunomodulatory and Tumor-Targeted Activity. Front Oncol. 2020 Dec 7;10:598477.
• [3] MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
• [4] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [5] Clinical pipeline report, company report or official report of Ono Pharmaceutical.
• [6] National Cancer Institute Drug Dictionary (drug name RXDX106).
• [7] The MERTK/FLT3 inhibitor MRX-2843 overcomes resistance-conferring FLT3 mutations in acute myeloid leukemia. JCI Insight. 2016 Mar;1(3):e85630.
• [8] National Cancer Institute Drug Dictionary (drug name PF-07265807).
• [9] The E3 ligase Cbl-b and TAM receptors regulate cancer metastasis via natural killer cells. Nature. 2014 Mar 27;507(7493):508-12.
• [10] G-749, a novel FLT3 kinase inhibitor, can overcome drug resistance for the treatment of acute myeloid leukemia. Blood. 2014 Apr 3;123(14):2209-19.
• [11] MerTK as a therapeutic target in glioblastoma. Neuro Oncol. 2018 Jan 10;20(1):92-102.
• [12] UNC569, a novel small-molecule mer inhibitor with efficacy against acute lymphoblastic leukemia in vitro and in vivo. Mol Cancer Ther. 2013 Nov;12(11):2367-77.
• [13] Company report (Mirati Therapeutics: formerly MethylGene)
• [14] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [15] AXL Targeting Abrogates Autophagic Flux and Induces Immunogenic Cell Death in Drug-Resistant Cancer Cells. J Thorac Oncol. 2020 Jun;15(6):973-999.
• [16] 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: 1835).
• [17] Clinical pipeline report, company report or official report of BioAtla
• [18] Enapotamab vedotin, an AXL-specific antibody-drug conjugate, shows preclinical antitumor activity in non-small cell lung cancer. JCI Insight. 2019 Nov 1;4(21):e128199.