Methotrexate (MTX; alphamethopterin; amethopterin; methylaminopterin; CL-14377; NCIC04671; WR19039; NCI-C04671) is an FDA approved antineoplastic and immunosuppressant drug that belongs to the antimetabolite and antifolate class of drugs.

Pemetrexed Disodium Hydrate (LY-231514; HSDB-7316; trade name Alimta), the hydrated disodium salt of Pemetrexed which is a synthetic pyrimidine-based antifolate, is a novel antifolate and antimetabolite anticancer drug targeting TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively.

Aminopterin (4-Aminofolic acid; APGA) is a novel and synthetic folic acid derivative used as a rodenticide that has been shown to be teratogenic, but whose metabolite is a competitive inhibitor of dihydrofolate reductase, which is a cofactor for nucleic acid synthesis.

Pralatrexate (PDX; trade name Folotyn), an antifolate which is structurally a folate analog, is a potent and selective inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities.

Sulfameter (Bayrena; Sulfametoxydiazine; 5-Methoxysulfadiazine; NSC-683528; I-2586; SH-613) is a novel, long-acting sulfonamide antibacterial agent used as a leprostatic agent and also is used to treat UTIs/urinary tract infections.

Pyrimethamine (Malocid; Khloridin; BW 50-63; NCI-C01683; BW50-63; Daraprim; NSC 3061; Tindurin; WR-297; RP-4753) is a potent dihydrofolate reductase (DHFR) inhibitor which is used as an antimalarial and antiprotozoal drug.

Leucovorin calcium, a reduced folic acid and an active metabolite of folic acid, is a derivative of folic acid which can be used to increase levels of folic acid under conditions favoring folic acid inhibition.

Leucovorin calcium, a reduced folic acid and an active metabolite of folic acid (also known as folinic acid and citrovorum factor), is a derivative of folic acid which can be used to increase levels of folic acid under conditions favoring folic acid inhibition.