Pemetrexed

DB00642

small molecule approved investigational

Deskripsi

Pemetrexed is a chemotherapy drug that is manufactured and marketed by Eli Lilly and Company under the brand name Alimta. It is indicated for use in combination with cisplatin for the treatment of patients with malignant pleural mesothelioma whose disease is either unresectable or who are otherwise not candidates for curative surgery. Its use in non-small cell lung cancer has also been investigated. Pemetrexed was first approved by the FDA in February 4, 2004.A253907

Struktur Molekul 2D

Berat 427.4106
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of pemetrexed is 3.5 hours in patients with normal renal function (creatinine clearance of 90 mL/min).[L43807]
Volume Distribusi Pemetrexed has a steady-state volume of distribution of 16.1 liters.[L43807]
Klirens (Clearance) The total systemic clearance of pemetrexed is 91.8 mL/min in patients with normal renal function (creatinine clearance of 90 mL/min). As renal function decreases, the clearance of pemetrexed decreases, and exposure (AUC) of pemetrexed increases.[L43807]

Absorpsi

The pharmacokinetics of pemetrexed when pemetrexed was administered as a single agent in doses ranging from 0.2 to 838 mg/m2 infused over a 10-minute period have been evaluated in 426 cancer patients with a variety of solid tumors. Pemetrexed total systemic exposure (AUC) and maximum plasma concentration (Cmax) increased proportionally with the increase in dose. The pharmacokinetics of pemetrexed did not change over multiple treatment cycles.L43807

Metabolisme

Pemetrexed is not metabolized to an appreciable extent by the liver.L43807,A253987

Rute Eliminasi

Pemetrexed is primarily eliminated in the urine, with 70% to 90% of the dose recovered unchanged within the first 24 hours following administration. In vitro studies indicated that pemetrexed is a substrate of OAT3 (organic anion transporter 3), a transporter that is involved in the active secretion of pemetrexed.L43807

Interaksi Makanan

2 Data
  • 1. Administer folic acid supplement. Folic acid supplement of 400 to 1000 mcg daily should be given 7 days before treatment with pemetrexed and continued until 21 days after discontinuation of pemetrexed to reduce the risk of hematologic and gastrointestinal toxicities.
  • 2. Administer vitamin supplements. Administration of vitamin B12 intramuscular supplement one week before treatment with pemetrexed and every three cycles will reduce the risk of hematological and gastrointestinal toxicities.

Interaksi Obat

1405 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Pemetrexed.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Pemetrexed.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Pemetrexed.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Pemetrexed.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Pemetrexed.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Pemetrexed.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Pemetrexed.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Pemetrexed.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Pemetrexed.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Pemetrexed.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Pemetrexed.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Pemetrexed.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Pemetrexed.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Pemetrexed.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Pemetrexed.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Pemetrexed.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Pemetrexed.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Pemetrexed.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Pemetrexed.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Pemetrexed.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Pemetrexed.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Pemetrexed.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Pemetrexed.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Pemetrexed.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Pemetrexed.
Cladribine Pemetrexed may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Pemetrexed.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Pemetrexed.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Pemetrexed.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Pemetrexed.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Pemetrexed.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Pemetrexed.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Pemetrexed.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Pemetrexed.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Pemetrexed.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Pemetrexed.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Pemetrexed.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Pemetrexed.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Pemetrexed.
Sorafenib The risk or severity of adverse effects can be increased when Sorafenib is combined with Pemetrexed.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Pemetrexed.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Pemetrexed.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Pemetrexed.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Pemetrexed.
Teniposide The risk or severity of adverse effects can be increased when Teniposide is combined with Pemetrexed.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Pemetrexed.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Pemetrexed.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Pemetrexed.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Pemetrexed.
Zidovudine Zidovudine may decrease the excretion rate of Pemetrexed which could result in a higher serum level.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Pemetrexed.
Cyclophosphamide The risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Pemetrexed.
Vincristine The risk or severity of adverse effects can be increased when Vincristine is combined with Pemetrexed.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Pemetrexed.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Pemetrexed.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Pemetrexed.
Carbamazepine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Pemetrexed.
Vinblastine The risk or severity of adverse effects can be increased when Vinblastine is combined with Pemetrexed.
Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Pemetrexed.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Pemetrexed.
Linezolid Linezolid may decrease the excretion rate of Pemetrexed which could result in a higher serum level.
Imatinib The risk or severity of adverse effects can be increased when Imatinib is combined with Pemetrexed.
Triamcinolone The risk or severity of adverse effects can be increased when Triamcinolone is combined with Pemetrexed.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Pemetrexed.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Pemetrexed.
Fludrocortisone The risk or severity of adverse effects can be increased when Pemetrexed is combined with Fludrocortisone.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Pemetrexed is combined with Mycophenolate mofetil.
Daunorubicin The risk or severity of adverse effects can be increased when Pemetrexed is combined with Daunorubicin.
Irinotecan The risk or severity of adverse effects can be increased when Pemetrexed is combined with Irinotecan.
Methimazole The risk or severity of adverse effects can be increased when Pemetrexed is combined with Methimazole.
Etoposide The risk or severity of adverse effects can be increased when Pemetrexed is combined with Etoposide.
Dacarbazine The risk or severity of adverse effects can be increased when Pemetrexed is combined with Dacarbazine.
Temozolomide The risk or severity of adverse effects can be increased when Pemetrexed is combined with Temozolomide.
Penicillamine The risk or severity of adverse effects can be increased when Pemetrexed is combined with Penicillamine.
Prednisolone The risk or severity of adverse effects can be increased when Pemetrexed is combined with Prednisolone.
Sirolimus The risk or severity of adverse effects can be increased when Pemetrexed is combined with Sirolimus.
Mechlorethamine The risk or severity of adverse effects can be increased when Pemetrexed is combined with Mechlorethamine.
Azacitidine The risk or severity of adverse effects can be increased when Pemetrexed is combined with Azacitidine.
Methylprednisolone The risk or severity of adverse effects can be increased when Pemetrexed is combined with Methylprednisolone.
Dactinomycin The risk or severity of adverse effects can be increased when Pemetrexed is combined with Dactinomycin.
Cytarabine The risk or severity of adverse effects can be increased when Pemetrexed is combined with Cytarabine.
Azathioprine The risk or severity of adverse effects can be increased when Pemetrexed is combined with Azathioprine.
Doxorubicin The risk or severity of adverse effects can be increased when Pemetrexed is combined with Doxorubicin.
Hydroxyurea The risk or severity of adverse effects can be increased when Pemetrexed is combined with Hydroxyurea.
Busulfan The risk or severity of adverse effects can be increased when Pemetrexed is combined with Busulfan.
Mycophenolic acid The risk or severity of adverse effects can be increased when Pemetrexed is combined with Mycophenolic acid.
Topotecan The risk or severity of adverse effects can be increased when Pemetrexed is combined with Topotecan.
Mercaptopurine Mercaptopurine may decrease the excretion rate of Pemetrexed which could result in a higher serum level.
Thalidomide The risk or severity of adverse effects can be increased when Pemetrexed is combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Pemetrexed is combined with Melphalan.
Fludarabine The risk or severity of adverse effects can be increased when Pemetrexed is combined with Fludarabine.
Flucytosine The risk or severity of adverse effects can be increased when Pemetrexed is combined with Flucytosine.
Capecitabine The risk or severity of adverse effects can be increased when Pemetrexed is combined with Capecitabine.
Trilostane The risk or severity of adverse effects can be increased when Pemetrexed is combined with Trilostane.
Procarbazine The risk or severity of adverse effects can be increased when Pemetrexed is combined with Procarbazine.
Arsenic trioxide The risk or severity of adverse effects can be increased when Pemetrexed is combined with Arsenic trioxide.
Idarubicin The risk or severity of adverse effects can be increased when Pemetrexed is combined with Idarubicin.
Ifosfamide The risk or severity of adverse effects can be increased when Pemetrexed is combined with Ifosfamide.
Estramustine The risk or severity of adverse effects can be increased when Pemetrexed is combined with Estramustine.
Mitoxantrone The risk or severity of adverse effects can be increased when Pemetrexed is combined with Mitoxantrone.

Target Protein

Thymidylate synthase TYMS
Thymidylate synthase TMP1
Bifunctional purine biosynthesis protein ATIC ATIC
Dihydrofolate reductase DHFR
Trifunctional purine biosynthetic protein adenosine-3 GART

Referensi & Sumber

Artikel (PubMed)
  • PMID: 16291410
    Rollins KD, Lindley C: Pemetrexed: a multitargeted antifolate. Clin Ther. 2005 Sep;27(9):1343-82.
  • PMID: 17845983
    Lansiaux A, Lokiec F: Pemetrexed: from preclinic to clinic. Bull Cancer. 2007;94 Spec No Actualites:S134-8.
  • PMID: 20446853
    Fuld AD, Dragnev KH, Rigas JR: Pemetrexed in advanced non-small-cell lung cancer. Expert Opin Pharmacother. 2010 Jun;11(8):1387-402. doi: 10.1517/14656566.2010.482560.
  • PMID: 12722874
    Adjei AA: Pemetrexed (Alimta): a novel multitargeted antifolate agent. Expert Rev Anticancer Ther. 2003 Apr;3(2):145-56.
  • PMID: 15477632
    Hazarika M, White RM, Johnson JR, Pazdur R: FDA drug approval summaries: pemetrexed (Alimta). Oncologist. 2004;9(5):482-8. doi: 10.1634/theoncologist.9-5-482.
  • PMID: 22044606
    Sehouli J, Alvarez AM, Manouchehrpour S, Ghatage P, Szczylik C, Zimmermann A, Bauknecht T, Look KY, Oskay-Oezcelik G: A phase II trial of pemetrexed in combination with carboplatin in patients with recurrent ovarian or primary peritoneal cancer. Gynecol Oncol. 2012 Feb;124(2):205-9. doi: 10.1016/j.ygyno.2011.09.007. Epub 2011 Nov 1.
  • PMID: 30121390
    Gbolahan OB, Porter RF, Salter JT, Yiannoutsos C, Burns M, Chiorean EG, Loehrer PJ Sr: A Phase II Study of Pemetrexed in Patients with Recurrent Thymoma and Thymic Carcinoma. J Thorac Oncol. 2018 Dec;13(12):1940-1948. doi: 10.1016/j.jtho.2018.07.094. Epub 2018 Aug 16.
  • PMID: 25429526
    Choi YJ, Lee SH, Lee JL, Ahn JH, Lee KH, You D, Hong B, Hong JH, Ahn H: Phase II study of pemetrexed in combination with cisplatin in patients with advanced urothelial cancer: the PECULIAR study (KCSG 10-17). Br J Cancer. 2015 Jan 20;112(2):260-5. doi: 10.1038/bjc.2014.591. Epub 2014 Nov 27.
Menampilkan 8 dari 10 artikel.

Contoh Produk & Brand

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