antifolate

Lometrexol (LY 264618), an antipurine Antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and Apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.

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.

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.

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

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.

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

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.

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

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

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

Methotrexate disodium is an tetrahydrofolate dehydrogenase inhibitor

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

Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor, suppressing the growth of T. gondii strains with a TgDHFR IC50 of 1.57 ± 0.11 nM, a hDHFR IC50 of 308 ± 71 nM, and a hDHFR to TgDHFR selectivity ratio of 196.

Trimethoprim lactate (NSC-106568 lactate) is an antibiotic that inhibits bacterial dihydrofolate reductase (DHFR). Trimethoprim lactate has demonstrated antimicrobial activity, with excellent inhibition of Gramnegative bacteria. Trimethoprim lactate is used alone for the Trimethoprim lactate is used alone or in combination with other antibiotics to treat a variety of eye, lung, and gastrointestinal infections.

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.

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.

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.

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