Antifolate

Folinic acid calcium (Leucovorin Calcium) is the active metabolite of folic acid. Leucovorin is used principally as an antidote to folic acid antagonists.

Folinic Acid Calcium Salt Pentahydrate (Leucovorin Calcium Pentahydrate), a reduced folic acid, is used in combination with other chemotherapeutics.

Trimethoprim (NSC-106568) is a Dihydrofolate Reductase Inhibitor Antibacterial. The mechanism of action of trimethoprim is as a Dihydrofolate Reductase Inhibitor, and Cytochrome P450 2C8 Inhibitor, and Organic Cation Transporter 2 Inhibitor.

Methotrexate (WR19039) is a folate analog, an inhibitor of the dihydrofolate reductase DHFR. Methotrexate has antimetabolic, antitumor, and immunosuppressive activities, and is commonly used in rheumatoid arthritis and various tumors.

Diaveridine (AI3-23935) (DVD) is a popular antibacterial synergist that is widely used in combination with sulfonamide. It has been reported to be genotoxic to mammalian cells, but more studies are required to clarify this.

Levoleucovorin Calcium (CL307782), a calcium salt of the folinic acid, is used in cancer chemotherapy as an adjuvant.

Methotrexate disodium is an tetrahydrofolate dehydrogenase inhibitor

Pralatrexate (10-Propargyl-10-deazaaminopterin) is a folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities.

Calcium N5-methyltetrahydrofolate (NSC-173328) is the calcium salt of levomefolic acid, which has been proposed for treatment of cardiovascular disease and advanced cancers such as breast and colorectal cancers

Farletuzumab (MORAb-003) is a humanized monoclonal antibody with a high affinity for folate receptor-α (FRα), acting as a potent inhibitor of FRα and impeding the growth of cells that overexpress this receptor, making it useful for cancer research.

Mirvetuximab (M9346A) is a novel folate receptor α (FRα) monoclonal antibody targeting anti-FOLR1 (folate receptor 1). Mirvetuximab soravtansine is often conjugated with platinum compounds or other compounds to form antibody-drug conjugates for the treatment of ovarian cancer and other FRα-positive cancers.

Aminopterin (4-Aminofolic acid) is a synthetic folic acid derivative whose metabolite is a competitive inhibitor of dihydrofolate reductase

DHFR-IN-3 (7-bromoquinazoline-2,4-diamine) is a dihydrofolate reductase (DHFR) inhibitor.

Antifolate C2 (AGF 154) has antitumor activity with an IC of 0.14 nM measured in a growth inhibition assay of human tumor cells.Antifolate C2 can be used for the study of cancer and autoimmune diseases.

Antifolate C1 is an inhibitor of de novo purine biosynthesis. Antifolate C1 has selectivity for cellular uptake by high affinity folate receptors and the proton-coupled folate transporter (PCFT) over the reduced folate carrier (RFC).

FR-β ligand 1 (III) is a ligand that specifically targets folate receptors, exhibiting antitumor activity, high selectivity, and strong affinity.

Mirvetuximab soravtansine (IMGN853) is an antibody-drug coupling (ADC) targeting folate receptor alpha (FRα), which inhibits cell growth and enhances the antiproliferative effects of DNA damage, and may be useful in the study of drug-resistant ovarian cancer.

Opugotamig is a chimeric antibody of the half-IG G1 -κ/(scFv -κ-heavy) -h-CH2-CH3 type, specifically targeting FOLR1.

Rinatabart is a humanized IgG1κ antibody that targets FOLR1. The corresponding isotype control is HumanIgG1kappa, Isotype Control.

Mirvetuximab-DM4 (M9346A-DM4) is a compound targeting FOLR1 with potential anti-cancer activity. It can be used to synthesize Mirvetuximab soravtansine and study ovarian cancer.

Torvutatug is a human IgG1κ monoclonal antibody that acts against FOLR1.

FRα-targeting peptide C7 TFA is a selective peptide ligand for the folate receptor alpha (FRα) that specifically binds to FRα-expressing cells and has tumor-targeting capabilities in vivo. It is applicable in research related to tumor diagnosis and therapy.

Methotrexate metabolite (DAMPA) (DAMPA) is the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist. Methotrexate is used as a chemotherapeutic agent and immunosuppressant.

Pemetrexed (LY-231514 Disodium Hydrate), a guanine-derived antineoplastic agent, binds to and inhibits the enzyme thymidylate synthase (TS).