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

General Information of DTT (ID: TTPMQSO)

• DTT Name: ALK tyrosine kinase receptor (ALK) DTT Info
• UniProt ID: ALK_HUMAN
• Gene Name: ALK

Molecule-Related Drug & Molecule List

6 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Alectinib	DMP1I6Y	Lung cancer	2C25.0	Approved	[1]
Brigatinib	DM7W94S	Anaplastic large cell lymphoma	2A90.A	Approved	[2]
Ceritinib	DMB920Z	Non-small-cell lung cancer	2C25.Y	Approved	[3]
Crizotinib	DM4F29C	Non-small-cell lung cancer	2C25.Y	Approved	[4]
Entrectinib	DMMPTLH	Non-small cell lung cancer	2C25	Approved	[5]
Lorlatinib	DMICDLV	Non-small-cell lung cancer	2C25.Y	Approved	[6]

7 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ensartinib	DMIKDCQ	Non-small-cell lung cancer	2C25.Y	Phase 3	[7]
AP26113	DMYBQEF	Solid tumour/cancer	2A00-2F9Z	Phase 2	[8]
PF-06463922	DMKM7EW	Non-small-cell lung cancer	2C25.Y	Phase 2	[9]
TPX-0005	DM9FB2T	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[7]
TSR-011	DMFOR9Y	Non-small-cell lung cancer	2C25.Y	Phase 1/2	[10], [11]
X-396	DMZ9VCF	Advanced solid tumour	2A00-2F9Z	Phase 1/2	[12]
ASP3026	DMW72NJ	Diffuse large B-cell lymphoma	2A81	Phase 1	[13]

4 Patented Agent(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
1,2,4-triazolo[1,5a]pyridine derivative 2	DMZFILT	N. A.	N. A.	Patented	[14]
Benzimidazole derivative 6	DMV7TMB	Solid tumour/cancer	2A00-2F9Z	Patented	[15]
Carboxamide derivative 4	DMU5GKC	N. A.	N. A.	Patented	[16]
PMID28270010-Compound-Figure21-b	DM6IYAT	Brain metastases	2D50	Patented	[15]

12 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AZD3463	DMAX9C3	Discovery agent	N.A.	Investigative	[17]
CEP-18050	DMCIOSM	Lymphoma	2A80-2A86	Investigative	[17]
CEP-28122	DMAY04M	Solid tumour/cancer	2A00-2F9Z	Investigative	[17]
CRL-37212	DMERKU2	Solid tumour/cancer	2A00-2F9Z	Investigative	[17]
DLX-521	DMPD2XF	Discovery agent	N.A.	Investigative	[17]
GSK-1838705A	DM4HLK3	Discovery agent	N.A.	Investigative	[18]
PMID20483621C5g	DMQ918T	Discovery agent	N.A.	Investigative	[19]
PMID20483621C5m	DML6OZR	Discovery agent	N.A.	Investigative	[19]
PMID20483621C5n	DM2BUKP	Discovery agent	N.A.	Investigative	[19]
PMID22564207C25b	DMBMYKQ	Discovery agent	N.A.	Investigative	[20]
PMID24432909C8e	DMEGAZS	Discovery agent	N.A.	Investigative	[21]
PMID24900237C15	DM6TFPY	Discovery agent	N.A.	Investigative	[22]

References

• [1] CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011 May 17;19(5):679-90.
• [2] 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
• [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. (Ligand id: 7397).
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [6] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [7] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [8] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [9] PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models. Cancer Cell. 2015 Jul 13;28(1):70-81.
• [10] Treatment of ALK-positive non-small cell lung cancer. Arch Pathol Lab Med. 2012 Oct;136(10):1201-4.
• [11] National Cancer Institute Drug Dictionary (drug id 757983).
• [12] Clinical pipeline report, company report or official report of Xcovery.
• [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. (Ligand id: 7740).
• [14] Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 1.Expert Opin Ther Pat. 2017 Feb;27(2):127-143.
• [15] Tropomyosin receptor kinase inhibitors: an updated patent review for 2010-2016 - Part I.Expert Opin Ther Pat. 2017 Jun;27(6):733-751.
• [16] RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.
• [17] 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: 1839).
• [18] GSK1838705A inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers. Mol Cancer Ther. 2009 Oct;8(10):2811-20.
• [19] Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase. Bioorg Med Chem. 2010 Jun 15;18(12):4351-62.
• [20] Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase. J Med Chem. 2012 May 24;55(10):4580-93.
• [21] Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. J Med Chem.> 2014 Feb 27;57(4):1170-87.
• [22] Discovery of a potent inhibitor of anaplastic lymphoma kinase with in vivo antitumor activity. ACS Med Chem Lett. 2010 Sep 1;1(9):493-8.