Peringatan Keamanan

The oral LD50 is 1045 mg/kg in mice and 867 mg/kg in rats.L50196

In clinical trials involving patients with various cancers, single doses of up to 750 mg/m2 of irinotecan were associated with similar adverse events reported with the recommended dosage and regimen. There have been reports of overdosage at doses up to approximately twice the recommended therapeutic dose, which may be fatal. The most significant adverse reactions reported were severe neutropenia and severe diarrhea. Because there is no known antidote for overdosage of irinotecan, maximum supportive care should be instituted to prevent dehydration due to diarrhea and to treat any infectious complications.L50181

Irinotecan

DB00762

small molecule approved investigational

Deskripsi

Irinotecan is a topoisomerase inhibitor used for chemotherapy. It is a water-soluble analogue of camptothecin, which is extracted from the Chinese tree Camptotheca acuminate.A263376 The bis-piperidine side chain in the structure of irinotecan bestows enhanced water solubility.A263381 As an anticancer drug, irinotecan was first commercially available in Japan in 1994 to treat various cancers such as lung, cervical and ovarian cancer.A263376 Approved by the FDA in 1996,A263366 irinotecan is used to treat colorectal cancer and pancreatic adenocarcinoma.L50181, L50186, L50201 Irinotecan liposome was approved by the FDA in February 2024.L50186

The active metabolite SN-38 is also a potent inhibitor of DNA topoisomerase I. Both irinotecan and SN-38 mediate antitumor activity by forming a complex with topoisomerase?I and blocking its enzymatic activity, thereby interfering with DNA synthesis. This leads to the arrest of the cell cycle in the S-G2 phase and cancer cell death.A263376

Struktur Molekul 2D

Berat 586.678
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) After intravenous infusion of irinotecan in humans, the mean terminal elimination half-life of irinotecan is about 6 to 12 hours. The mean terminal elimination half-life of the active metabolite SN-38 is about 10 to 20 hours.[L50181]
Volume Distribusi Following intravenous infusion in patients with solid tumours, the mean (± standard deviation) volume of distribution of terminal elimination phase was 110 ± 48.5 L/m<sup>2</sup> at a dose of 125 mg/m<sup>2</sup> and 234 ± 69.6 L/m<sup>2</sup> at a dose of 340 mg/m<sup>2</sup>.[L50181]
Klirens (Clearance) The mean (± standard deviation) total systemic clearance of irinotecan in patients with solid tumours was 13.3 ± 6.01 L/h/m<sup>2</sup> at a dose of 125 mg/m<sup>2</sup> and 13.9 ± 4.0 L/h/m<sup>2</sup> at a dose of 340 mg/m<sup>2</sup>.[L50181]

Absorpsi

Over the recommended dose range of 50 to 350 mg/m2, the AUC of irinotecan increases linearly with dose; the AUC of SN-38 increases less than proportionally with dose. Maximum concentrations of the active metabolite SN-38 are generally seen within 1 hour following the end of a 90-minute infusion of irinotecan.L50181 The plasma levels of SN-38 are much lower than that of irinotecan.A1169, L50181 Following intravenous infusion in patients with solid tumours, the mean (± standard deviation) Cmax was 1,660 ± 797 ng/mL at a dose of 125 mg/m2 and 3,392 ± 874 ng/mL at a dose of 340 mg/m2. The AUC0–24 was 10,200 ± 3,270 ng x h/mL at a dose of 125 mg/m2 and 20,604 ± 6,027 ng x h/mL at a dose of 340 mg/m2.L50181

Metabolisme

Upon administration, irinotecan is converted primarily in the liver into its active metabolite, SN-38, by carboxylesterase.A263366 SN-38 is formed by cleavage of the carbamate bond between the camptothecin moiety and the dipiperidino side chain.L50181 While in vitro cytotoxicity assays show that the potency of SN-38 relative to irinotecan varies, SN-38 is approximately 1000 times as potent as irinotecan as an inhibitor of topoisomerase I.A1169, L50181 SN-38 can further be glucuronidated by UGT1A1 to form SN-38G.A1168, A263366, L50181 Irinotecan can also undergo CYP3A4-mediated oxidation to form NPC and APC. While some sources state that NPC and APC are weak inhibitors of topoisomerase I,A1168, A1169 they are unlikely to contribute to the pharmacological activity of irinotecan.

Rute Eliminasi

The disposition of irinotecan has not been fully elucidated in humans. The urinary excretion of irinotecan, SN-38, and SN-38 glucuronide are 11% to 20%, <1%, and 3%, respectively. The cumulative biliary and urinary excretion of irinotecan and its metabolites (SN-38 and SN-38 glucuronide) over a period of 48 hours in two patients ranged from approximately 25% (100 mg/m2) to 50% (300 mg/m2).L50181

Farmakogenomik

5 Varian
SLCO1B1 (rs4149056)

Patients with this genotype have reduced transport of the active metabolite of irinotecan resulting in increased plasma concentrations.

UGT1A1 (rs8175347)

The presence of this genotype in UGT1A1 may indicate an increased risk of bone marrow toxicity when treated with irinotecan.

UGT1A7 (rs17868323)

The presence of this genotype in UGT1A1 may indicate an increased risk of bone marrow toxicity when treated with irinotecan.

UGT1A1 (rs10929302)

The presence of this genotype in UGT1A1 may indicate an increased risk of bone marrow toxicity when treated with irinotecan.

UGT1A1 (rs8175347)

Patients who carry this genotype in UGT1A1 are at increased risk for neutropenia following initiation of irinotecan treatment.

Interaksi Obat

1107 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Irinotecan.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Irinotecan.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Irinotecan.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Irinotecan.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Irinotecan.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Irinotecan.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Irinotecan.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Irinotecan.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Irinotecan.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Irinotecan.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Irinotecan.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Irinotecan.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Irinotecan.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Irinotecan.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Irinotecan.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Irinotecan.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Irinotecan.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Irinotecan.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Irinotecan.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Irinotecan.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Irinotecan.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Irinotecan.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Irinotecan.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Irinotecan.
Cladribine Irinotecan may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Irinotecan.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Irinotecan.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Irinotecan.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Irinotecan.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Irinotecan.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Irinotecan.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Irinotecan.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Irinotecan.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Irinotecan.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Irinotecan.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Irinotecan.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Irinotecan.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Irinotecan.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Irinotecan.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Irinotecan.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Irinotecan.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Irinotecan.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Irinotecan.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Irinotecan.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Irinotecan.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Irinotecan.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Irinotecan.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Irinotecan.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Irinotecan.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Irinotecan.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Irinotecan.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Irinotecan.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Irinotecan.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Irinotecan.
Tretinoin The metabolism of Irinotecan can be decreased when combined with Tretinoin.
Sulfasalazine The risk or severity of adverse effects can be increased when Irinotecan is combined with Sulfasalazine.
Dacarbazine The risk or severity of adverse effects can be increased when Irinotecan is combined with Dacarbazine.
Temozolomide The risk or severity of adverse effects can be increased when Irinotecan is combined with Temozolomide.
Penicillamine The risk or severity of adverse effects can be increased when Irinotecan is combined with Penicillamine.
Mechlorethamine The risk or severity of adverse effects can be increased when Irinotecan is combined with Mechlorethamine.
Azacitidine The risk or severity of adverse effects can be increased when Irinotecan is combined with Azacitidine.
Carboplatin The risk or severity of adverse effects can be increased when Irinotecan is combined with Carboplatin.
Dactinomycin The risk or severity of adverse effects can be increased when Irinotecan is combined with Dactinomycin.
Cytarabine The risk or severity of adverse effects can be increased when Irinotecan is combined with Cytarabine.
Azathioprine The risk or severity of adverse effects can be increased when Irinotecan is combined with Azathioprine.
Hydroxyurea The risk or severity of adverse effects can be increased when Irinotecan is combined with Hydroxyurea.
Mycophenolic acid The risk or severity of adverse effects can be increased when Irinotecan is combined with Mycophenolic acid.
Mercaptopurine The risk or severity of adverse effects can be increased when Irinotecan is combined with Mercaptopurine.
Thalidomide The metabolism of Irinotecan can be increased when combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Irinotecan is combined with Melphalan.
Fludarabine The risk or severity of adverse effects can be increased when Irinotecan is combined with Fludarabine.
Flucytosine The risk or severity of adverse effects can be increased when Irinotecan is combined with Flucytosine.
Capecitabine The risk or severity of adverse effects can be increased when Irinotecan is combined with Capecitabine.
Trilostane The risk or severity of adverse effects can be increased when Irinotecan is combined with Trilostane.
Procarbazine The risk or severity of adverse effects can be increased when Irinotecan is combined with Procarbazine.
Arsenic trioxide The risk or severity of adverse effects can be increased when Irinotecan is combined with Arsenic trioxide.
Idarubicin The risk or severity of adverse effects can be increased when Irinotecan is combined with Idarubicin.
Estramustine The risk or severity of adverse effects can be increased when Irinotecan is combined with Estramustine.
Lomustine The risk or severity of adverse effects can be increased when Irinotecan is combined with Lomustine.
Eculizumab The risk or severity of adverse effects can be increased when Irinotecan is combined with Eculizumab.
Decitabine The risk or severity of adverse effects can be increased when Irinotecan is combined with Decitabine.
Nelarabine The risk or severity of adverse effects can be increased when Irinotecan is combined with Nelarabine.
Ciclesonide The risk or severity of adverse effects can be increased when Irinotecan is combined with Ciclesonide.
Stepronin The risk or severity of adverse effects can be increased when Irinotecan is combined with Stepronin.
Hydroxychloroquine The risk or severity of adverse effects can be increased when Irinotecan is combined with Hydroxychloroquine.
Castanospermine The risk or severity of adverse effects can be increased when Irinotecan is combined with Castanospermine.
Vorinostat The risk or severity of adverse effects can be increased when Irinotecan is combined with Vorinostat.
2-Methoxyethanol The risk or severity of adverse effects can be increased when Irinotecan is combined with 2-Methoxyethanol.
Brequinar The risk or severity of adverse effects can be increased when Irinotecan is combined with Brequinar.
Thiotepa The risk or severity of adverse effects can be increased when Irinotecan is combined with Thiotepa.
Aldosterone The risk or severity of adverse effects can be increased when Irinotecan is combined with Aldosterone.
Ixabepilone The risk or severity of adverse effects can be increased when Irinotecan is combined with Ixabepilone.
Pirfenidone The risk or severity of adverse effects can be increased when Irinotecan is combined with Pirfenidone.
Belinostat The risk or severity of adverse effects can be increased when Irinotecan is combined with Belinostat.
Trabectedin The risk or severity of adverse effects can be increased when Irinotecan is combined with Trabectedin.
Interferon alfa The risk or severity of adverse effects can be increased when Irinotecan is combined with Interferon alfa.
Glatiramer The risk or severity of adverse effects can be increased when Irinotecan is combined with Glatiramer.
Briakinumab The risk or severity of adverse effects can be increased when Irinotecan is combined with Briakinumab.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Irinotecan is combined with Human interferon omega-1.
Panobinostat The risk or severity of adverse effects can be increased when Irinotecan is combined with Panobinostat.

Target Protein

DNA topoisomerase I, mitochondrial TOP1MT
DNA topoisomerase 1 TOP1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 19852077
    Ramesh M, Ahlawat P, Srinivas NR: Irinotecan and its active metabolite, SN-38: review of bioanalytical methods and recent update from clinical pharmacology perspectives. Biomed Chromatogr. 2010 Jan;24(1):104-23. doi: 10.1002/bmc.1345.
  • PMID: 9342501
    Chabot GG: Clinical pharmacokinetics of irinotecan. Clin Pharmacokinet. 1997 Oct;33(4):245-59.
  • PMID: 11161230
    Rothenberg ML: Irinotecan (CPT-11): recent developments and future directions--colorectal cancer and beyond. Oncologist. 2001;6(1):66-80. doi: 10.1634/theoncologist.6-1-66.
  • PMID: 32119328
    Reyhanoglu G, Smith T: Irinotecan. .
  • PMID: 26604633
    Fujita K, Kubota Y, Ishida H, Sasaki Y: Irinotecan, a key chemotherapeutic drug for metastatic colorectal cancer. World J Gastroenterol. 2015 Nov 21;21(43):12234-48. doi: 10.3748/wjg.v21.i43.12234.
  • PMID: 32664667
    Kciuk M, Marciniak B, Kontek R: Irinotecan-Still an Important Player in Cancer Chemotherapy: A Comprehensive Overview. Int J Mol Sci. 2020 Jul 12;21(14):4919. doi: 10.3390/ijms21144919.

Contoh Produk & Brand

Produk: 79 • International brands: 2
Produk
  • Camptosar
    Injection, solution • 20 mg/1mL • Intravenous • US • Approved
  • Camptosar
    Injection, solution • 20 mg/1mL • Intravenous • US • Approved
  • Camptosar
    Solution • 20 mg / mL • Intravenous • Canada • Approved
  • Camptosar
    Injection, solution • 20 mg/1mL • Intravenous • US • Approved
  • Camptosar
    Injection, solution • 20 mg/1mL • Intravenous • US • Approved
  • Irinotecan
    Solution • 20 mg / mL • Intravenous • Canada • Approved
  • Irinotecan for Injection
    Solution • 20 mg / mL • Intravenous • Canada • Approved
  • Irinotecan hydrochloide
    Injection • 20 mg/1mL • Intravenous • US • Generic • Approved
Menampilkan 8 dari 79 produk.
International Brands
  • Biotecan
  • Campto — YakultHonsha Co. Ltd.

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