Peringatan Keamanan

The LD50 of intravenous trimetrexate in mice is 62 mg/kg (186 mg/m2). Myelosuppression is a dose-limiting toxic effect.

Trimetrexate

DB01157

small molecule approved investigational

Deskripsi

A nonclassical folic acid inhibitor through its inhibition of the enzyme dihydrofolate reductase. It is being tested for efficacy as an antineoplastic agent and as an antiparasitic agent against pneumocystis pneumonia in AIDS patients. Myelosuppression is its dose-limiting toxic effect.

Struktur Molekul 2D

Berat 369.4176
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 11 to 20 hours
Volume Distribusi * 20 ± 8 L/m2 * 36.9 ± 6 L/m2 [cancer patients]
Klirens (Clearance) * 38 +/- 15 mL/min/m2 [patients with acquired immunodeficiency syndrome (AIDS) who had Pneumocystis carinii pneumonia (4 patients) or toxoplasmosis (2 patients). Trimetrexate was administered intravenously as a bolus injection at a dose of 30 mg/m2/day along with leucovorin 20 mg/m2 every 6 hours for 21 days] * 53 +/- 41 mL/min/m2 [Cancer patients with advanced solid tumors using various dosage regimensreceiving a single-dose administration of 10 to 130 mg/m2] * 30 +/- 8 mL/min/m2 [Cancer patients with advanced solid tumors using various dosage regimensafter a five-day infusion]

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Hepatic. Preclinical data strongly suggest that the major metabolic pathway is oxidative O-demethylation, followed by conjugation to either glucuronide or the sulfate.

Rute Eliminasi

Ten to 30% of the administered dose is excreted unchanged in the urine.

Interaksi Obat

770 Data
Tetrahydrofolic acid The therapeutic efficacy of Trimetrexate can be decreased when used in combination with Tetrahydrofolic acid.
Folic acid The therapeutic efficacy of Trimetrexate can be decreased when used in combination with Folic acid.
Leucovorin The therapeutic efficacy of Trimetrexate can be decreased when used in combination with Leucovorin.
(6S)-5,6,7,8-tetrahydrofolic acid The therapeutic efficacy of Trimetrexate can be decreased when used in combination with (6S)-5,6,7,8-tetrahydrofolic acid.
Triglu-5-formyl-tetrahydrofolate The therapeutic efficacy of Trimetrexate can be decreased when used in combination with Triglu-5-formyl-tetrahydrofolate.
Levoleucovorin The therapeutic efficacy of Trimetrexate can be decreased when used in combination with Levoleucovorin.
5-methyltetrahydrofolic acid The therapeutic efficacy of Trimetrexate can be decreased when used in combination with 5-methyltetrahydrofolic acid.
Cyclosporine Cyclosporine may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Methotrexate Methotrexate may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cephalexin Cephalexin may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Meloxicam The risk or severity of methemoglobinemia can be increased when Trimetrexate is combined with Meloxicam.
Carprofen Carprofen may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Tacrolimus Tacrolimus may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Ibuprofen Ibuprofen may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Atazanavir Atazanavir may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefoperazone Cefoperazone may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefotetan Cefotetan may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefoxitin Cefoxitin may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Ceftizoxime Ceftizoxime may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefradine Cefradine may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Magnesium salicylate Magnesium salicylate may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Salsalate Salsalate may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Choline magnesium trisalicylate Choline magnesium trisalicylate may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefepime Cefepime may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefacetrile Cefacetrile may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Ceftibuten Ceftibuten may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cefpodoxime Cefpodoxime may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Antrafenine Antrafenine may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Aminophenazone Aminophenazone may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Antipyrine Antipyrine may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Tiaprofenic acid Tiaprofenic acid may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Lopinavir Lopinavir may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Etoricoxib Etoricoxib may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Hydrolyzed Cephalothin Hydrolyzed Cephalothin may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Cephalothin Group Cephalothin Group may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Oxyphenbutazone Oxyphenbutazone may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Latamoxef Latamoxef may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Nimesulide Nimesulide may decrease the excretion rate of Trimetrexate which could result in a higher serum level.
Benoxaprofen Benoxaprofen may decrease the excretion rate of Trimetrexate which could result in a higher serum level.

Target Protein

Peptide deformylase, mitochondrial PDF
Dihydrofolate reductase DHFR

Referensi & Sumber

Synthesis reference: Martin Stogniew, Javad M. Zadei, "Compositions comprising trimetrexate and methods of their synthesis and use." U.S. Patent US6258821, issued January, 1974.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Neutrexin
    Injection, powder, lyophilized, for solution • 200 mg/16mL • Intravenous • US • Approved
  • Neutrexin
    Injection, powder, lyophilized, for solution • 25 mg/2mL • Intravenous • US • Approved
  • Neutrexin Pws IV 25mg/vial
    Powder, for solution • 25 mg / vial • Intravenous • Canada • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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