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Literature DB >> 3157662

Trimetrexate: a new antifol entering clinical trials.

P J O'Dwyer, D D Shoemaker, J Plowman, J Cradock, A Grillo-Lopez, B Leyland-Jones.

Abstract

Trimetrexate, a 2,4-diaminoquinazoline derivative, is a new antifol recently introduced into clinical trials. It differs from methotrexate principally in its transport (not carrier-mediated), and its intracellular retention (not polyglutamylated). Trimetrexate is active against tumors which are methotrexate-resistant on the basis of impaired transport, and has a broader range of antitumor activity in preclinical models. Animal studies predict toxicity principally to the central nervous system, gastrointestinal tract and bone marrow.

Entities: Chemical Disease

Mesh：

Substances：

Year: 1985 PMID： 3157662 DOI： 10.1007/bf00176828

Source DB: PubMed Journal: Invest New Drugs ISSN： 0167-6997 Impact factor: 3.850

12 in total

1. Membrane transport considerations in high-dose methotrexate regimens with leucovorin rescue.

Authors: I D Goldman
Journal: Cancer Treat Rep Date: 1981

Review 2. The pharmacology and clinical use of methotrexate.

Authors: J Jolivet; K H Cowan; G A Curt; N J Clendeninn; B A Chabner
Journal: N Engl J Med Date: 1983-11-03 Impact factor: 91.245

3. Growth inhibitory, transport and biochemical properties of the gamma-glutamyl and gamma-aspartyl peptides of methotrexate in L1210 leukemia cells in vitro.

Authors: F M Sirotnak; P L Chello; J R Piper; J A Montgomery
Journal: Biochem Pharmacol Date: 1978 Impact factor: 5.858

4. Pharmacology and toxicity of a potent "nonclassical" 2,4-diamino quinazoline folate antagonist, trimetrexate, in normal dogs.

Authors: E C Weir; A R Cashmore; R N Dreyer; M L Graham; N Hsiao; B A Moroson; W L Sawicki; J R Bertino
Journal: Cancer Res Date: 1982-05 Impact factor: 12.701

5. Uptake and efficacy of trimetrexate (TMQ, 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl] quinazoline), a non-classical antifolate in methotrexate-resistant leukemia cells in vitro.

Authors: B A Kamen; B Eibl; A Cashmore; J Bertino
Journal: Biochem Pharmacol Date: 1984-05-15 Impact factor: 5.858

6. In situ methotrexate polyglutamate formation in rat tissues.

Authors: G R Krakower; B A Kamen
Journal: J Pharmacol Exp Ther Date: 1983-12 Impact factor: 4.030

7. Intracellular pharmacokinetics of methotrexate polyglutamates in human breast cancer cells. Selective retention and less dissociable binding of 4-NH2-10-CH3-pteroylglutamate4 and 4-NH2-10-CH3-pteroylglutamate5 to dihydrofolate reductase.

Authors: J Jolivet; B A Chabner
Journal: J Clin Invest Date: 1983-09 Impact factor: 14.808

8. Folate antagonists. 20. Synthesis and antitumor and antimalarial properties of trimetrexate and related 6-[(phenylamino)methyl]-2,4-quinazolinediamines.

Authors: E F Elslager; J L Johnson; L M Werbel
Journal: J Med Chem Date: 1983-12 Impact factor: 7.446

9. Patterns of cross-resistance to the antifolate drugs trimetrexate, metoprine, homofolate, and CB3717 in human lymphoma and osteosarcoma cells resistant to methotrexate.

Authors: H Diddens; D Niethammer; R C Jackson
Journal: Cancer Res Date: 1983-11 Impact factor: 12.701

10. Enzymatic assays for 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl]quinazoline, a promising new "nonclassical" antifolate.

Authors: J J Heusner; J J McCormack
Journal: J Pharm Sci Date: 1981-07 Impact factor: 3.534

9 in total

1. Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate.

Authors: Alexis Nzila; Matthias Rottmann; Penchit Chitnumsub; Stevens M Kiara; Sumalee Kamchonwongpaisan; Cherdsak Maneeruttanarungroj; Supannee Taweechai; Bryan K S Yeung; Anne Goh; Suresh B Lakshminarayana; Bin Zou; Josephine Wong; Ngai Ling Ma; Margaret Weaver; Thomas H Keller; Veronique Dartois; Sergio Wittlin; Reto Brun; Yongyuth Yuthavong; Thierry T Diagana
Journal: Antimicrob Agents Chemother Date: 2010-03-29 Impact factor: 5.191

2. Skin reactions induced by trimetrexate, an analog of methotrexate.

Authors: R B Weiss; W D James; W B Major; M B Porter; C J Allegra; G A Curt
Journal: Invest New Drugs Date: 1986 Impact factor: 3.850

Review 3. Clinical pharmacokinetics and pharmacology of trimetrexate.

Authors: J L Marshall; R J DeLap
Journal: Clin Pharmacokinet Date: 1994-03 Impact factor: 6.447

4. A phase I trial of trimetrexate glucuronate (NSC 352122) given every 3 weeks: clinical pharmacology and pharmacodynamics.

Authors: L B Grochow; D A Noe; D S Ettinger; R C Donehower
Journal: Cancer Chemother Pharmacol Date: 1989 Impact factor: 3.333

Review 5. Biological and biochemical properties of new anticancer folate antagonists.

Authors: D W Fry; R C Jackson
Journal: Cancer Metastasis Rev Date: 1987 Impact factor: 9.264

6. A phase I study of trimetrexate, an analog of methotrexate, administered monthly in the form of nine consecutive daily bolus injections.

Authors: J Jolivet; L Landry; M F Pinard; J J McCormack; W P Tong; E Eisenhauer
Journal: Cancer Chemother Pharmacol Date: 1987 Impact factor: 3.333