Raltitrexed Folic acid

Raltitrexed is a folic acid analogue which inhibits thymidylate synthetase. Intracellularly formed raltitrexed polyglutamates are even stronger inhibitors of thymidylate synthetase than the parent compound. Similar to methotrexate polyglutamates... 

Folic acid analogs methotrexate sodium raltitrexed disodium... 

Folic acid antagonists methotrexate, raltitrexed. Purine derivatives cladribine (2-chlorodeoxyadeno-sine), fludarabine, mercaptopurine, pentostatin (deoxycoformycin), tioguanine. 

Because folic acid and many of its analogs are hydrophilic, they cross the blood—brain barrier poorly and require specific transport mechanisms to enter mammalian cells. Three inward folate transport systems are found on mammalian cells (I) a folate receptor, which has high (fffin-ity for folic acid but much reduced ability to transport methotrexate and other analogs (2) the reduced folate transporter, the majortransitproteinfor methotrexate, raltitrexed, pemetrexed, and most... 

The antimetabolite, raltitrexed, is a folate analogue and is a potent and specific inhibitor of the enzyme thymidylate synthase. Inhibition of this enzyme ultimately interferes with the synthesis of deoxyribonucleic acid (DNA) leading to cell death. The intracellular polyglutamation of raltitrexed leads to the formation within cells of even more potent inhibitors of thymidylate synthase. Folate (methylene tetrahydrofolate) is a co-faetor required by thymidylate synthase and therefore theoretically folinic acid or folic acid may interfere with the aetion of raltitrexed. Clinieal interaction studies have not yet been undertaken to confirm these predieted inter-aetions. ... 

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See also in sourсe #XX -- [ ]

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