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

General Information of Drug (ID: DM1DISM)

• Drug Name: MDAM (y-methylene-10-deazaaminopterin) Drug Info

Indication

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

• Cross-matching ID: TTD Drug ID: DM1DISM

Molecule-Related Drug Atlas

Drug(s) Targeting Dihydrofolate reductase (DHFR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Trimethoprim	DMM7CHK	Acute otitis media	AB00	Approved	[3]
Aminosalicylic Acid	DMENSL5	Crohn disease	DD70	Approved	[3]
Leucovorin Calcium	DMNWZJG	Solid tumour/cancer	2A00-2F9Z	Approved	[4]
Methotrexate Sodium	DM5XH2C	Solid tumour/cancer	2A00-2F9Z	Approved	[3]
Iclaprim	DM7YNV9	Bacterial infection	1A00-1C4Z	Phase 3	[5]
PIRITREXIM	DM276N1	Bladder cancer	2C94	Phase 2	[6]
CH-4051	DMLQRYH	Rheumatoid arthritis	FA20	Phase 2	[7]
L-MDAM	DMU901D	Solid tumour/cancer	2A00-2F9Z	Phase 1	[8]
VYR 006	DMC9N7D	Toxoplasmosis	1F57	Phase 1	[9]
TNP-351	DMW05DS	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 2	[10]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Dihydrofolate reductase (DHFR)	TTYZVDJ	DYR_HUMAN	Inhibitor	[2]

References

• [1] Final results of a phase I and pharmacokinetic study of gamma-methylene-10-deazaaminopterin (MDAM) administered intravenously daily for five consec... Cancer Chemother Pharmacol. 2004 May;53(5):370-6.
• [2] Evaluation of the importance of hydrophobic interactions in drug binding to dihydrofolate reductase. J Med Chem. 1988 Jan;31(1):129-37.
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [4] Biochemical factors in the selectivity of leucovorin rescue: selective inhibition of leucovorin reactivation of dihydrofolate reductase and leucovorin utilization in purine and pyrimidine biosynthesis by methotrexate and dihydrofolate polyglutamates.NCI Monogr.1987;(5):17-26.
• [5] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [6] Structural variations of piritrexim, a lipophilic inhibitor of human dihydrofolate reductase: synthesis, antitumor activity and molecular modeling ... Eur J Med Chem. 2004 Dec;39(12):1079-88.
• [7] CH-1504, a metabolically inert antifolate for the potential treatment of rheumatoid arthritis. IDrugs. 2010 Aug;13(8):559-67.
• [8] Polyglutamylation of the dihydrofolate reductase inhibitor gamma-methylene-10-deazaaminopterin is not essential for antitumor activity. Clin Cancer Res. 1996 Apr;2(4):707-12.
• [9] Clinical pipeline report, company report or official report of Vyera Pharmaceuticals.
• [10] A Ring-Transformation/Ring-Annulation Strategy for the Synthesis of the DHFR Inhibitor, TNP-351: A Correction. J Org Chem. 1996 Nov 1;61(22):7973-7974.