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

General Information of Drug (ID: DMPGEO1)

• Drug Name: BrP-LPA Drug Info
• Synonyms: alpha-bromomethylene phosphonate

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 16725999
  TTD Drug ID: DMPGEO1

Molecule-Related Drug Atlas

Drug(s) Targeting Lysophosphatidic acid receptor 2 (LPAR2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LPA	DMI5XR1	Discovery agent	N.A.	Investigative	[2]
Ki16425	DMJTDK9	Discovery agent	N.A.	Investigative	[3]
2-oleoyl-LPA	DMN9OS1	Discovery agent	N.A.	Investigative	[4]
dodecyl-thiophosphate	DMAJVPI	Discovery agent	N.A.	Investigative	[5]
oleoyl-thiophosphate	DM1TAM9	Discovery agent	N.A.	Investigative	[5]
NAEPA	DM38XWZ	Discovery agent	N.A.	Investigative	[6]
dodecylphosphate	DMPCLTW	Discovery agent	N.A.	Investigative	[7]
PMID18178086C15	DMA2OWK	Discovery agent	N.A.	Investigative	[8]
decyl dihydrogen phosphate	DMNKDT5	Discovery agent	N.A.	Investigative	[7]
GRI977143	DM3A0TE	Discovery agent	N.A.	Investigative	[9]

Drug(s) Targeting Lysophosphatidic acid receptor 1 (LPAR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SAR-100842	DMDMQW0	Fibrosis	GA14-GC01	Phase 2	[10]
BMS-986020	DMHMV6E	Scleroderma	4A42	Phase 2	[11]
BMS-986278	DMD27RW	Pulmonary fibrosis	CB03.4	Phase 2	[12]
BMS-986337	DM9GC6L	Pulmonary fibrosis	CB03.4	Phase 1	[13]
BMS-986202	DM8TAI9	Idiopathic pulmonary fibrosis	CB03.4	Preclinical	[14]
LPA	DMI5XR1	Discovery agent	N.A.	Investigative	[15]
Ki16425	DMJTDK9	Discovery agent	N.A.	Investigative	[16]
dioctanoylglycerol pyrophosphate	DM0QY1V	Discovery agent	N.A.	Investigative	[17]
2-oleoyl-LPA	DMN9OS1	Discovery agent	N.A.	Investigative	[4]
dodecyl-thiophosphate	DMAJVPI	Discovery agent	N.A.	Investigative	[5]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Lysophosphatidic acid receptor 1 (LPAR1)	TTQ6S1K	LPAR1_HUMAN	Antagonist	[1]
Lysophosphatidic acid receptor 2 (LPAR2)	TTB7Y8I	LPAR2_HUMAN	Antagonist	[1]

References

• [1] 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.
• [2] Synthesis and biological evaluation of phosphonic and thiophosphoric acid derivatives of lysophosphatidic acid. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3473-6.
• [3] Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors. Mol Pharmacol. 2003 Oct;64(4):994-1005.
• [4] 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.
• [5] 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.
• [6] LPA and its analogs-attractive tools for elucidation of LPA biology and drug development. Curr Med Chem. 2008;15(21):2122-31.
• [7] Fatty alcohol phosphates are subtype-selective agonists and antagonists of lysophosphatidic acid receptors. Mol Pharmacol. 2003 May;63(5):1032-42.
• [8] Discovery of potent LPA2 (EDG4) antagonists as potential anticancer agents. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1037-41.
• [9] Virtual screening for LPA2-specific agonists identifies a nonlipid compound with antiapoptotic actions. Mol Pharmacol. 2012 Dec;82(6):1162-73.
• [10] Promising Pharmacological Directions in the World of Lysophosphatidic Acid Signaling. Biomol Ther (Seoul) 2015 January; 23(1): 1-11.
• [11] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [12] 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.
• [13] 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.
• [14] Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. J Pharmacol Exp Ther. 2011 Mar;336(3):693-700.
• [15] Diversity of lysophosphatidic acid receptor-mediated intracellular calcium signaling in early cortical neurogenesis. J Neurosci. 2010 May 26;30(21):7300-9.
• [16] 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.
• [17] Short-chain phosphatidates are subtype-selective antagonists of lysophosphatidic acid receptors. Mol Pharmacol. 2001 Oct;60(4):776-84.