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Antimetabolite and fluoropyrimidine regimens

22 articles

7+3 chemotherapy

7+3 chemotherapy is the standard intensive induction regimen for acute myeloid leukemia, combining 7 days of continuous-infusion cytarabine with 3 days of daunorubicin or idarubicin.

Aminopterin

Aminopterin, also known as 4-aminofolic acid, is a synthetic folic acid analog that in 1948 became the first drug to induce remissions in childhood leukemia.

Arfolitixorin

Arfolitixorin (6R-MTHF, Modufolin, Rescufolin) is an investigational direct-acting folate from Isofol Medical that potentiates 5-FU; its phase III AGENT trial in metastatic colorectal cancer failed to show superiority over leucovorin.

Azacitidine/venetoclax regimen

The azacitidine/venetoclax regimen pairs azacitidine with the BCL-2 inhibitor venetoclax to treat newly diagnosed acute myeloid leukemia in adults 75 or older or unfit for intensive chemotherapy.

Capecitabine and gemcitabine regimen

The capecitabine and gemcitabine regimen (GEM-CAP, CapGem) is a doublet chemotherapy combining oral capecitabine with intravenous gemcitabine, used to treat advanced pancreatic and biliary tract cancers.

Cytarabine and daunorubicin regimen

The cytarabine and daunorubicin regimen, known as 7+3, combines seven days of cytarabine with three days of daunorubicin and is standard induction therapy for acute myeloid leukemia.

Doxifluridine

Doxifluridine (5'-DFUR, Furtulon, Ro 21-9738) is an oral fluoropyrimidine prodrug of 5-fluorouracil activated by thymidine phosphorylase; capecitabine is its liver-derived successor prodrug.

Floxuridine

Floxuridine, also called FUDR, is a fluorinated pyrimidine antimetabolite chemotherapy drug, FDA-approved in 1970 and given by continuous hepatic artery infusion, mainly for colorectal cancer that has spread to the liver.

Folitixorin

Folitixorin (5,10-methylenetetrahydrofolate; CoFactor, ANX-510) is a folate-based biomodulator, INN 8881, UNII 0SXY5ET48B, that stabilizes FdUMP binding to thymidylate synthase to potentiate 5-fluorouracil; its [6R] isomer arfolitixorin failed superiority over leucovorin in the phase III AGENT trial.

Fosgemcitabine palabenamide

Fosgemcitabine palabenamide (NUC-1031, Acelarin) is an investigational ProTide prodrug of gemcitabine for cancer, designed to bypass hENT1 transport, dCK activation, and CDA breakdown; its phase III biliary tract trial missed its survival endpoint.

Gemcitabine and irinotecan regimen

The Gemcitabine and irinotecan regimen is a combination chemotherapy doublet studied in advanced pancreatic cancer; phase III results showed no significant survival benefit over gemcitabine monotherapy.

Gemcitabine and vinorelbine regimen

The gemcitabine and vinorelbine regimen is a two-drug combination chemotherapy pairing gemcitabine with vinorelbine, studied mainly in metastatic breast cancer, non-small-cell lung cancer, and recurrent ovarian cancer.

Gemcitabine monotherapy regimen

Gemcitabine monotherapy is a chemotherapy regimen in which gemcitabine is given intravenously alone, approved in 1996 for advanced pancreatic cancer and now mainly used in elderly or frail patients.

Gimeracil

Gimeracil (CDHP, 5-chloro-2,4-dihydroxypyridine), a DPD inhibitor in the oral anticancer drug S-1/Teysuno with tegafur and oteracil (1:0.4:1), prolongs 5-FU activity for gastric and colorectal cancer.

Infusional fluorouracil and leucovorin regimen

The infusional fluorouracil and leucovorin regimen is a chemotherapy combination giving 5-fluorouracil by continuous intravenous infusion with leucovorin, used chiefly to treat colorectal and other cancers.

Methotrexate and vinblastine regimen

The methotrexate and vinblastine regimen is a two-drug intravenous chemotherapy combination used mainly for advanced urothelial carcinoma and desmoid-type fibromatosis, and forms the backbone of MVAC.

Methotrexate regimen

A methotrexate regimen is a dosing protocol for the antifolate drug methotrexate, given alone or with other agents to treat cancers, rheumatoid arthritis, and psoriasis, with doses spanning several thousand-fold.

Nelarabine

Nelarabine (Arranon, Atriance) is a purine nucleoside analog prodrug of ara-G for T-cell acute lymphoblastic leukemia and lymphoma, converted by adenosine deaminase; FDA-approved 2005 for relapsed/refractory disease and 2023 for frontline use.

Nolatrexed

Nolatrexed (AG337, Thymitaq) is a nonclassical lipophilic quinazoline thymidylate synthase inhibitor, not polyglutamated, that reached phase III hepatocellular carcinoma trials but was refused FDA approval in 2005.

Oteracil

Oteracil (potassium oxonate, oxonic acid) is the OPRT-inhibiting gastrointestinal-protective component of S-1 (tegafur/gimeracil/oteracil, TS-1, Teysuno), combined in a 1:0.4:1 molar ratio to reduce 5-FU gut toxicity.

Sapacitabine

Sapacitabine (CS-682, CYC682) is an oral nucleoside analogue prodrug of CNDAC that induces DNA strand breaks; it reached phase 3 trials in elderly AML (SEAMLESS) but failed its primary endpoint and development was discontinued in 2023.

Tegafur

Tegafur, also known as ftorafur, is an oral fluoropyrimidine prodrug of the anticancer drug 5-fluorouracil, given in combinations such as UFT and S-1 for gastric, colorectal, and breast cancers.