Peringatan Keamanan

The oral LD50 is 333 mg/kg in mice and >500 mg/kg in rats. The dermal LD50 in rabbits is >1000 mg/kg.L33005

There is no known antidote for gemcitabine overdose. In a dose-escalation study, patients were administered a single dose of gemcitabine as high as 5700 mg/m2 administered by intravenous infusion over 30 minutes every two weeks: main observed toxicities were myelosuppression, paresthesia, and severe rash. In the event of a suspected drug overdose, blood counts should be monitored, and patients should be provided with supportive therapy, as necessary.L32950

Gemcitabine

DB00441

small molecule approved

Deskripsi

Gemcitabine is a nucleoside analog and a chemotherapeutic agent. It was originally investigated for its antiviral effects, but it is now used as an anticancer therapy for various cancers.A233135 Gemcitabine is a cytidine analog with two fluorine atoms replacing the hydroxyl on the ribose.A233145 As a prodrug, gemcitabine is transformed into its active metabolites that work by replacing the building blocks of nucleic acids during DNA elongation, arresting tumour growth and promoting apoptosis of malignant cells.L32960 The structure, metabolism, and mechanism of action of gemcitabine are similar to cytarabine, but gemcitabine has a wider spectrum of antitumour activity.A233140

Gemcitabine is marketed as Gemzar and it is available as intravenous injection. It is approved by the FDA to treat advanced ovarian cancer in combination with carboplatin, metastatic breast cancer in combination with paclitaxel, non-small cell lung cancer in combination with cisplatin, and pancreatic cancer as monotherapy.L32950 It is also being investigated in other cancer and tumour types.

Struktur Molekul 2D

Berat 263.1981
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following intravenous infusions lasting less than 70 minutes, the terminal half-life ranged from 0.7 to 1.6 hours. Following infusions ranging from 70 to 285 minutes, the terminal half-life ranged from 4.1 to 10.6 hours.[L32960] Females tend to have longer half-lives than male patients. Gemcitabine triphosphate, the active metabolite of gemcitabine, can accumulate in circulating peripheral blood mononuclear cells. The terminal half-life of gemcitabine triphosphate, the active metabolite, from mononuclear cells ranges from 1.7 to 19.4 hours.[L32950]
Volume Distribusi In patients with various solid tumours, the volume of distribution increased with infusion length. The volume of distribution of gemcitabine was 50 L/m<sup>2</sup> following infusions lasting less than 70 minutes. For long infusions, the volume of distribution rose to 370 L/m<sup>2</sup>.[L32950] Gemcitabine triphosphate, the active metabolite of gemcitabine, accumulates and retains in solid tumour cells _in vitro_ and _in vivo_. It is not extensively distributed to tissues after short infusions that last less than 70 minutes.[A233140] It is not known whether gemcitabine crosses the blood-brain barrier, but gemcitabine is widely distributed into tissues, including ascitic fluid.[L32960] In rats, placental and lacteal transfer occurred rapidly at five to 15 minutes following drug administration.[A233135]
Klirens (Clearance) Following intravenous infusions lasting less than 70 minutes, clearance ranged from 41 to 92 L/h/m<sup>2</sup> in males and ranged from 31 to 69 L/h/m<sup>2</sup> in females.[L32960] Clearance decreases with age. Females have about 30% lower clearance than male patients.[L32950]

Absorpsi

Peak plasma concentrations of gemcitabine range from 10 to 40 mg/L following a 30-minute intravenous infusion, and are reached at 15 to 30 minutes. One study showed that steady-state concentrations of gemcitabine showed a linear relationship to dose over the dose range 53 to 1000 mg/m2. Gemcitabine triphosphate, the active metabolite of gemcitabine, can accumulate in circulating peripheral blood mononuclear cells. In one study, the Cmax of gemcitabine triphosphate in peripheral blood mononuclear cells occurred within 30 minutes of the end of the infusion period and increased increased proportionally with gemcitabine doses of up to 350 mg/m2.A233140

Metabolisme

Following administration and uptake into cancer cells, gemcitabine is initially phosphorylated by deoxycytidine kinase (dCK), and to a lower extent, the extra-mitochondrial thymidine kinase 2 to form gemcitabine monophosphate (dFdCMP). dFdCMP is subsequently phosphorylated by nucleoside kinases to form active metabolites, gemcitabine diphosphate (dFdCDP) and gemcitabine triphosphate (dFdCTP).A233145 Gemcitabine is also deaminated intracellularly and extracellularly by cytidine deaminase to its inactive metabolite 2?,2?-difluorodeoxyuridine or 2´-deoxy-2´,2´-difluorouridine (dFdU). Deamination occurs in the blood, liver, kidneys, and other tissues,A233135 and this metabolic pathway accounts for most of drug clearance.A233145,L32960

Rute Eliminasi

Gemcitabine mainly undergoes renal excretion. Within a week following administration of a single dose of 1000 mg/m2 infused over 30 minutes, about 92-98% of the dose was recovered in urine where 89% of the recovered dose was excreted as difluorodeoxyuridine (dFdU) and less than 10% as gemcitabine.L32950 Monophosphate, diphosphate, or triphosphate metabolites of gemcitabine are not detectable in urine. In a single-dose study, about 1% of the administered dose was recovered in the feces.A233135

Farmakogenomik

1 Varian
RRM1 (rs9937)

Patients with this genotype have increased risk of neutropenia and neurotoxicity with gemcitabine.

Interaksi Obat

1344 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Gemcitabine.
Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Gemcitabine.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Gemcitabine.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Gemcitabine.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Gemcitabine.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Gemcitabine.
Anakinra The risk or severity of adverse effects can be increased when Anakinra is combined with Gemcitabine.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Gemcitabine.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Gemcitabine.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Gemcitabine.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Gemcitabine.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Gemcitabine.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Gemcitabine.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Gemcitabine.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Gemcitabine.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Gemcitabine.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Gemcitabine.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Gemcitabine.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Gemcitabine.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Gemcitabine.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Gemcitabine.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Gemcitabine.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Gemcitabine.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Gemcitabine.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Gemcitabine.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Gemcitabine.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Gemcitabine.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Gemcitabine.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Gemcitabine.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Gemcitabine.
Cladribine Gemcitabine may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Gemcitabine.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Gemcitabine.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Gemcitabine.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Gemcitabine.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Gemcitabine.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Gemcitabine.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Gemcitabine.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Gemcitabine.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Gemcitabine.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Gemcitabine.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Gemcitabine.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Gemcitabine.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Gemcitabine.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Gemcitabine.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Gemcitabine.
Betamethasone The risk or severity of adverse effects can be increased when Gemcitabine is combined with Betamethasone.
Teniposide The risk or severity of adverse effects can be increased when Gemcitabine is combined with Teniposide.
Epirubicin The risk or severity of adverse effects can be increased when Gemcitabine is combined with Epirubicin.
Chloramphenicol The risk or severity of adverse effects can be increased when Gemcitabine is combined with Chloramphenicol.
Lenalidomide The risk or severity of adverse effects can be increased when Gemcitabine is combined with Lenalidomide.
Altretamine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Altretamine.
Zidovudine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Zidovudine.
Cisplatin The risk or severity of adverse effects can be increased when Gemcitabine is combined with Cisplatin.
Oxaliplatin The risk or severity of adverse effects can be increased when Gemcitabine is combined with Oxaliplatin.
Cyclophosphamide The risk or severity of adverse effects can be increased when Gemcitabine is combined with Cyclophosphamide.
Vincristine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Vincristine.
Propylthiouracil The risk or severity of adverse effects can be increased when Gemcitabine is combined with Propylthiouracil.
Pentostatin The risk or severity of adverse effects can be increased when Gemcitabine is combined with Pentostatin.
Methotrexate The risk or severity of adverse effects can be increased when Gemcitabine is combined with Methotrexate.
Carbamazepine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Carbamazepine.
Vinblastine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Vinblastine.
Fluticasone propionate The risk or severity of adverse effects can be increased when Gemcitabine is combined with Fluticasone propionate.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Gemcitabine is combined with Fluocinolone acetonide.
Linezolid The risk or severity of adverse effects can be increased when Gemcitabine is combined with Linezolid.
Imatinib The risk or severity of adverse effects can be increased when Gemcitabine is combined with Imatinib.
Triamcinolone The risk or severity of adverse effects can be increased when Gemcitabine is combined with Triamcinolone.
Clofarabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Clofarabine.
Prednisone The risk or severity of adverse effects can be increased when Gemcitabine is combined with Prednisone.
Pemetrexed The risk or severity of adverse effects can be increased when Gemcitabine is combined with Pemetrexed.
Fludrocortisone The risk or severity of adverse effects can be increased when Gemcitabine is combined with Fludrocortisone.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Gemcitabine is combined with Mycophenolate mofetil.
Daunorubicin The risk or severity of adverse effects can be increased when Gemcitabine is combined with Daunorubicin.
Irinotecan The risk or severity of adverse effects can be increased when Gemcitabine is combined with Irinotecan.
Methimazole The risk or severity of adverse effects can be increased when Gemcitabine is combined with Methimazole.
Etoposide The risk or severity of adverse effects can be increased when Gemcitabine is combined with Etoposide.
Sulfasalazine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Sulfasalazine.
Dacarbazine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Dacarbazine.
Temozolomide The risk or severity of adverse effects can be increased when Gemcitabine is combined with Temozolomide.
Penicillamine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Penicillamine.
Prednisolone The risk or severity of adverse effects can be increased when Gemcitabine is combined with Prednisolone.
Sirolimus The risk or severity of adverse effects can be increased when Gemcitabine is combined with Sirolimus.
Mechlorethamine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Mechlorethamine.
Azacitidine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Azacitidine.
Carboplatin The risk or severity of adverse effects can be increased when Gemcitabine is combined with Carboplatin.
Methylprednisolone The risk or severity of adverse effects can be increased when Gemcitabine is combined with Methylprednisolone.
Dactinomycin The risk or severity of adverse effects can be increased when Gemcitabine is combined with Dactinomycin.
Cytarabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Cytarabine.
Azathioprine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Azathioprine.
Doxorubicin The risk or severity of adverse effects can be increased when Gemcitabine is combined with Doxorubicin.
Hydroxyurea The risk or severity of adverse effects can be increased when Gemcitabine is combined with Hydroxyurea.
Busulfan The risk or severity of adverse effects can be increased when Gemcitabine is combined with Busulfan.
Mycophenolic acid The risk or severity of adverse effects can be increased when Gemcitabine is combined with Mycophenolic acid.
Topotecan The risk or severity of adverse effects can be increased when Gemcitabine is combined with Topotecan.
Mercaptopurine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Mercaptopurine.
Thalidomide The risk or severity of adverse effects can be increased when Gemcitabine is combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Gemcitabine is combined with Melphalan.
Fludarabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Fludarabine.
Trilostane The risk or severity of adverse effects can be increased when Gemcitabine is combined with Trilostane.
Procarbazine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Procarbazine.

Target Protein

DNA
Ribonucleoside-diphosphate reductase subunit M2 RRM2
Ribonucleoside-diphosphate reductase large subunit RRM1
Thymidylate synthase TYMS
UMP-CMP kinase CMPK1

Referensi & Sumber

Synthesis reference: John A. Weigel, "Process for making gemcitabine hydrochloride." U.S. Patent US6001994, issued May, 1995.
Artikel (PubMed)
  • PMID: 9279506
    Noble S, Goa KL: Gemcitabine. A review of its pharmacology and clinical potential in non-small cell lung cancer and pancreatic cancer. Drugs. 1997 Sep;54(3):447-72. doi: 10.2165/00003495-199754030-00009.
  • PMID: 16555971
    Toschi L, Finocchiaro G, Bartolini S, Gioia V, Cappuzzo F: Role of gemcitabine in cancer therapy. Future Oncol. 2005 Feb;1(1):7-17. doi: 10.1517/14796694.1.1.7.
  • PMID: 27007129
    Ciccolini J, Serdjebi C, Peters GJ, Giovannetti E: Pharmacokinetics and pharmacogenetics of Gemcitabine as a mainstay in adult and pediatric oncology: an EORTC-PAMM perspective. Cancer Chemother Pharmacol. 2016 Jul;78(1):1-12. doi: 10.1007/s00280-016-3003-0. Epub 2016 Mar 23.

Contoh Produk & Brand

Produk: 139 • International brands: 23
Produk
  • Act Gemcitabine
    Powder, for solution • 200 mg / vial • Intravenous • Canada • Approved
  • Act Gemcitabine
    Powder, for solution • 1 g / vial • Intravenous • Canada • Approved
  • Act Gemcitabine
    Solution • 38 mg / mL • Intravenous • Canada • Approved
  • Aj-gemcitabine
    Powder, for solution • 200 mg / vial • Intravenous • Canada • Generic • Approved
  • Aj-gemcitabine
    Powder, for solution • 1 g / vial • Intravenous • Canada • Generic • Approved
  • Aj-gemcitabine
    Powder, for solution • 2 g / vial • Intravenous • Canada • Generic • Approved
  • Gemcitabine
    Injection, powder, lyophilized, for solution • 40 mg/1mL • Intravenous • US • Generic • Approved
  • Gemcitabine
    Injection, powder, lyophilized, for solution • 200 mg/5mL • Intravenous • US • Generic • Approved
Menampilkan 8 dari 139 produk.
International Brands
  • Abine — Dosa
  • Abingem — Miracalus
  • Acytabin — Intas
  • Celgem — Alkem
  • Celzar — Celon
  • Cytogem — Dr Reddys
  • Daplax — Dr Reddys
  • Dercin — Egis
  • Eriogem — Eriochem
  • Fotinex — Fada

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul