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

General Information of DTT (ID: TTQ6S1K)

• DTT Name: Lysophosphatidic acid receptor 1 (LPAR1) DTT Info
• Gene Name: LPAR1

Molecule-Related Drug & Molecule List

4 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BMS-986020	DMHMV6E	Scleroderma	4A42	Phase 2	[1]
BMS-986278	DMD27RW	Pulmonary fibrosis	CB03.4	Phase 2	[2]
SAR-100842	DMDMQW0	Fibrosis	GA14-GC01	Phase 2	[3]
BMS-986337	DM9GC6L	Pulmonary fibrosis	CB03.4	Phase 1	[4]

1 Preclinical Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BMS-986202	DM8TAI9	Idiopathic pulmonary fibrosis	CB03.4	Preclinical	[5]

32 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(1,1-Difluoro-pentadecyl)-phosphonic acid	DMDK59X	Discovery agent	N.A.	Investigative	[6]
2-oleoyl-LPA	DMN9OS1	Discovery agent	N.A.	Investigative	[7]
alkyl OMPT	DMM19AO	Discovery agent	N.A.	Investigative	[8]
anti-BrP-LPA	DM3IOR0	Discovery agent	N.A.	Investigative	[9]
BrP-LPA	DMPGEO1	Discovery agent	N.A.	Investigative	[9]
Decyl-phosphonic acid	DMFT3J2	Discovery agent	N.A.	Investigative	[6]
dioctanoylglycerol pyrophosphate	DM0QY1V	Discovery agent	N.A.	Investigative	[10]
Dodecyl-phosphonic acid	DMLHKI9	Discovery agent	N.A.	Investigative	[6]
dodecyl-thiophosphate	DMAJVPI	Discovery agent	N.A.	Investigative	[6]
Ki16425	DMJTDK9	Discovery agent	N.A.	Investigative	[11]
LPA	DMI5XR1	Discovery agent	N.A.	Investigative	[12]
NAEPA	DM38XWZ	Discovery agent	N.A.	Investigative	[13]
oleoyl-thiophosphate	DM1TAM9	Discovery agent	N.A.	Investigative	[14]
ONO-3080573	DM8LKED	Discovery agent	N.A.	Investigative	[15]
ONO-9780307	DMATXHR	Discovery agent	N.A.	Investigative	[15]
ONO-9910539	DML4DPV	Discovery agent	N.A.	Investigative	[15]
Phosphoric acid mono-((E)-dec-4-enyl) ester	DMS57HX	Discovery agent	N.A.	Investigative	[6]
Phosphoric acid mono-((E)-dodec-9-enyl) ester	DMC873V	Discovery agent	N.A.	Investigative	[6]
Phosphoric acid mono-((E)-tetradec-11-enyl) ester	DMET9ZC	Discovery agent	N.A.	Investigative	[6]
Phosphoric acid mono-((E)-tetradec-9-enyl) ester	DME8APC	Discovery agent	N.A.	Investigative	[6]
Phosphoric acid monodec-9-enyl ester	DMANVJY	Discovery agent	N.A.	Investigative	[6]
Phosphoric acid monododecyl ester	DMME0VN	Discovery agent	N.A.	Investigative	[6]
Phosphoric acid monotetradecyl ester	DMG5MJL	Discovery agent	N.A.	Investigative	[6]
syn-BrP-LPA	DMM5PVL	Discovery agent	N.A.	Investigative	[9]
T13	DMVRJEL	Discovery agent	N.A.	Investigative	[14]
Tetradecyl-phosphonic acid	DMABITD	Discovery agent	N.A.	Investigative	[6]
Thiophosphoric acid (E)-dodec-9-enyl ester	DMZ4FCB	Discovery agent	N.A.	Investigative	[6]
Thiophosphoric acid (E)-tetradec-9-enyl ester	DMYOXJ4	Discovery agent	N.A.	Investigative	[6]
Thiophosphoric acid dec-9-enyl ester	DM12NGE	Discovery agent	N.A.	Investigative	[6]
Thiophosphoric acid decyl ester	DM36KW9	Discovery agent	N.A.	Investigative	[6]
VPC12249	DM6F0VR	Discovery agent	N.A.	Investigative	[16]
VPC32183	DMLK3I9	Discovery agent	N.A.	Investigative	[17]

References

• [1] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [2] Phase 2 trial design of BMS-986278, a lysophosphatidic acid receptor 1 (LPA(1)) antagonist, in patients with idiopathic pulmonary fibrosis (IPF) or progressive fibrotic interstitial lung disease (PF-ILD). BMJ Open Respir Res. 2021 Dec;8(1):e001026.
• [3] Promising Pharmacological Directions in the World of Lysophosphatidic Acid Signaling. Biomol Ther (Seoul) 2015 January; 23(1): 1-11.
• [4] ClinicalTrials.gov (NCT04550195) A Double-Blind, Placebo-Controlled, Randomized, Single and Multiple Ascending Dose Study of the Safety and Tolerability, and Pharmacokinetics (Including Food Effect, pH Effect and Japanese Bridging Study) of BMS-986337 Following Oral Administration in Healthy Participants. U.S.National Institutes of Health.
• [5] Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. J Pharmacol Exp Ther. 2011 Mar;336(3):693-700.
• [6] Synthesis, structure-activity relationships, and biological evaluation of fatty alcohol phosphates as lysophosphatidic acid receptor ligands, activ... J Med Chem. 2005 Jul 28;48(15):4919-30.
• [7] Lysophosphatidic acid (LPA) receptors of the EDG family are differentially activated by LPA species. Structure-activity relationship of cloned LPA receptors. FEBS Lett. 2000 Jul 28;478(1-2):159-65.
• [8] Phosphorothioate analogues of alkyl lysophosphatidic acid as LPA3 receptor-selective agonists. ChemMedChem. 2006 Mar;1(3):376-83.
• [9] Dual activity lysophosphatidic acid receptor pan-antagonist/autotaxin inhibitor reduces breast cancer cell migration in vitro and causes tumor regression in vivo. Cancer Res. 2009 Jul 1;69(13):5441-9.
• [10] Short-chain phosphatidates are subtype-selective antagonists of lysophosphatidic acid receptors. Mol Pharmacol. 2001 Oct;60(4):776-84.
• [11] Targeting lysophosphatidic acid receptor type 1 with Debio 0719 inhibits spontaneous metastasis dissemination of breast cancer cells independently of cell proliferation and angiogenesis. Int J Oncol. 2012 Apr;40(4):1133-41.
• [12] Diversity of lysophosphatidic acid receptor-mediated intracellular calcium signaling in early cortical neurogenesis. J Neurosci. 2010 May 26;30(21):7300-9.
• [13] LPA and its analogs-attractive tools for elucidation of LPA biology and drug development. Curr Med Chem. 2008;15(21):2122-31.
• [14] Pharmacological tools for lysophospholipid GPCRs: development of agonists and antagonists for LPA and S1P receptors. Acta Pharmacol Sin. 2010 Sep;31(9):1213-22.
• [15] Crystal Structure of Antagonist Bound Human Lysophosphatidic Acid Receptor 1. Cell. 2015 Jun 18;161(7):1633-43.
• [16] Activity of 2-substituted lysophosphatidic acid (LPA) analogs at LPA receptors: discovery of a LPA1/LPA3 receptor antagonist. Mol Pharmacol. 2001 Dec;60(6):1173-80.
• [17] Initial structure-activity relationships of lysophosphatidic acid receptor antagonists: discovery of a high-affinity LPA1/LPA3 receptor antagonist. Bioorg Med Chem Lett. 2004 Jun 7;14(11):2735-40.