antifolate

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.

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.

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.

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).

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.

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.

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

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.

Methotrexate disodium is an tetrahydrofolate dehydrogenase inhibitor

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

Pyrimethamine (Pirimecidan) is a competitive inhibitor of dihydrofolate reductase (DHFR), used as an antimalarial drug.

Folinic acid (Leucovorin) is a biofolate used in the treatment of methotrexate (MTX) toxicity reduction and as an adjuvant therapy for colon cancer.

Levomefolate calcium, an artificial form of folate, is a coenzymated form of folic acid that offers a more bioavailable alternative in dietary supplements.

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

Pemetrexed disodium (LY-231514) is a parenterally administered folate antagonist and antineoplastic agent, used in the treatment of non-small cell lung cancer and malignant mesothelioma. Pemetrexed disodium therapy has been associated with moderate rates of serum enzyme elevations during therapy, but has not been convincingly linked to instances of acute, clinically apparent liver injury.

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

Metoprine is a potent inhibitor of histamine N-methyltransferase (HMT), with potential antineoplastic activity.

Pemetrexed disodium hemipenta hydrate (LY-231514 Disodium Hydrate) is a new-type antifolate and antimetabolite for TS, DHFR, and GARFT. The Ki of Pemetrexed Disodium Hydrate for TS, DHFR and GARFT is 1.3 nM, 7.2 nM and 65 nM, respectively.

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.

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

Proguanil hydrochloride (Chloroquanil) is a biguanide compound which metabolizes in the body to form cycloguanil, an anti-malaria agent.Upon hydrolysis, Proguanil hydrochloride is converted to its active cyclic triazine metabolite, cycloguanil, by a cytochrome P450 dependent reaction. Cycloguanil selectively inhibits the bifunctional dihydrofolate reductase-thymidylate synthase of plasmodium parasite, thereby disrupting deoxythymidylate synthesis and ultimately blocking DNA and protein synthesis in the parasite.