Literature DB >> 6974058

Phase I clinical trial and pharmacology of 2,4-diamino-5-(3',4'-dichlorophenyl)-6-methylpyrimidine (metoprine) (DDMP) and folinic acid (CF).

R de Jager, D Dupont, J J Rodzynek, C Dorlet, G Lagrange.   

Abstract

Escalating doses of DDMP (metoprine) (15-280 mg/m2) were administered as single oral doses 24 h before a fixed leucovorin (CF) rescue (15 mg IM every 6 h for 72 h). CNS toxicity was dose-limiting and cumulative when the drug was given more frequently than at 3-week intervals. DDMP has a very long half-life (150 h) and is extensively bound to serum proteins (88%). It diffuses into the CSF and concentrates in brain tumours and normal brain tissue (brainserum ratio 3.8-5.3). DDMP is a potentially useful drug against brain tumors. Tumor regressions were seen in two patients with epidermoid carcinomas.

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Year:  1981        PMID: 6974058     DOI: 10.1007/BF00253013

Source DB:  PubMed          Journal:  Cancer Chemother Pharmacol        ISSN: 0344-5704            Impact factor:   3.333


  21 in total

1.  Methotrexate resistance and uptake of DDMP by L5178Y cells. Selective protection with folinic acid.

Authors:  B T Hill; L A Price; J H Goldie; S I Harrison
Journal:  Eur J Cancer       Date:  1975-08       Impact factor: 9.162

2.  Folate transport by the choroid plexus in vitro.

Authors:  R Spector; A V Lorenzo
Journal:  Science       Date:  1975-02-14       Impact factor: 47.728

3.  Methodichlorophen as anti-tumor drug.

Authors:  L A Price; J H Goldie; B T Hill
Journal:  Br Med J       Date:  1975-04-05

4.  Treatment of meningeal leukemia with pyrimethamine.

Authors:  G F Geils; C W Scott; C M Baugh
Journal:  Blood       Date:  1971-08       Impact factor: 22.113

5.  Experimental chemotherapy with 5-arylpyrimidine antifolates: Further studies on toxicity and the responsiveness of ascitic, solid, and intracranial sarcoma 180 to DDMP and DDMP with citrovorum factor.

Authors:  F M Sirotnak; D M Moccio; D M Dorick
Journal:  Cancer Treat Rep       Date:  1977-10

6.  Dihydrofolate reductase in primary brain tumors, cell cultures of central nervous system origin, and normal brain during fetal and neonatal growth.

Authors:  D S Duch; D D Bigner; S W Bowers; C A Nichol
Journal:  Cancer Res       Date:  1979-02       Impact factor: 12.701

7.  Transport characteristics of folates in cerebrospinal fluid; a study utilizing doubly labeled 5-methyltetrahydrofolate and 5-formyltetrahydrofolate.

Authors:  M Levitt; P F Nixon; J H Pincus; J R Bertino
Journal:  J Clin Invest       Date:  1971-06       Impact factor: 14.808

8.  Studies with a 2,4-diamino-5-(3',4'-dichlorophenyl)-6-methylpyrimidine (DDMP)-resistant L1210 leukemia cell line without cross-resistance to methotrexate.

Authors:  G P Browman; C Gorka; C Mehta; H Lazarus; H T Abelson
Journal:  Biochem Pharmacol       Date:  1980-08-15       Impact factor: 5.858

9.  Identification of dihydrofolate reductase in human central-nervous-system tumours.

Authors:  H T Abelson; M Fosburg; C Gorka; P Kornblith
Journal:  Lancet       Date:  1978-01-28       Impact factor: 79.321

Review 10.  DDMP (2,4-diamino-5-(3',4'-dichlorophenyl)-methylpyrimidine).

Authors:  B T Hill; L A Price
Journal:  Cancer Treat Rev       Date:  1980-06       Impact factor: 12.111

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