Peringatan Keamanan

Overdose of vinflunine is associated with bone marrow suppression with a risk of severe infection. There is no known antidote for vinflunine overdose. In case of overdose, the vital functions of the patient should be closely monitored and other appropriate measures, such as blood transfusions and administration of antibiotics or growth factors, should be taken if necessary L2381. The severity of correlates with the AUC of, or overall exposure to, vinflunine L2381.

In the in vivo micronucleus test in rat, vinflunine was clastogenic that induced chromosome breakage. In a mouse lymphoma assay, vinflunine displayed mutagenic and clastogenic potential without any metabolic activation L2381. In the reproduction studies, vinflunine caused embryolethal and teratogenic effects in rabbits and teratogenic effects in rats. 2 cases of malformations of the uterus and vagina following vinflunine treatment were reported during the pre- and post-natal development study in rat L2381.

Vinflunine

DB11641

small molecule approved investigational

Deskripsi

Vinflunine is a third-generation member of the vinca alkaloid family with anti-tumour actions. It was first described in 1998 at the Pierre Fabre research center in France. Like other vinca agents, vinflunine is an anti-mitotic agent that induces a cell cycle arrest at the G2/M phase and promotes cell death via apoptosis L1396. Vinflunine is a microtubule inhibitor that binds to tubulin at or near to the vinca binding sites to inhibits its polymerization into microtubules during cell proliferation L1396. In murine tumors and human tumor xenografts, vinflunine exhibits an antitumor efficacy than DB00361, DB00570, and DB00541 A31975.

Having an incidence of 429,700 new cases per year worldwide, urothelial carcinoma of the bladder is one of the most common malignancies that mostly affects individuals aged 50–79 years A32626. Some patients with advanced urothelial carcinoma experience inadequate therapeutic response from a prior platinum-containing regimen. While these patients have a median survival of approximately 4 months and a poor prognosis L1396, there is currently no standard therapy in patients with advanced urothelial carcinoma A32626. In 2009, vinflunine was approved by the European Medicines Agency (EMA) as a second-line therapy of metastatic and advanced urothelial cancer after failure of platinum-based treatment A32626. Vinflunine ditartrate is an active ingredient in the EMA-authorised product Javlor for intravenous infusion. Efficacy and safety of vinflunine has not been studied in patients with performance status of 2 or less. The clinical use of vinflunine in other urologic malignancies, such as inoperable cancer of the penis, are currently have been investigated A32626.

Struktur Molekul 2D

Berat 816.944
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean terminal half-life is approximately 40 h [L2381]. The half life of the main metabolite, DVFL, is approximately 120 hours [L2381].
Volume Distribusi The terminal volume of distribution is large, 2422 ± 676 L (about 35 l/kg), suggesting extensive distribution into tissues. The ratio between plasma and whole blood concentrations of 0.80 ± 0.12 [L2381].
Klirens (Clearance) The total blood clearance was 40 L/h according to a population pharmacokinetic analysis in 372 patients. The inter- and intra-individual variability was low, with the coefficient of variation approximately 25% and 8%, respectively [L2381].

Absorpsi

Vinflunine displays a linear pharmacokinetic profile in the range of administered doses (from 30 mg/m^2 to 400 mg/m^2) in cancer patients L2381.

Metabolisme

The metabolites of influnine are mostly cytochrome P450 3A4, but 4-O-deacetylvinflunine (DVFL) may be slowly formed by multiple esterases. DVFL is the main metabolite and is the only metabolite that retains pharmacological activity L2381.

Rute Eliminasi

Fecal excretion accounts for 2/3 of the total elimination of vinflunine and its metabolites and the remaining 1/3 of their elimination indicates urinary excretion L2381.

Interaksi Makanan

2 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits CYP3A metabolism, which may increase the serum concentration of vinflunine.
  • 2. Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of vinflunine.

Interaksi Obat

643 Data
Modafinil The metabolism of Vinflunine can be increased when combined with Modafinil.
Armodafinil The metabolism of Vinflunine can be increased when combined with Armodafinil.
Ranolazine The serum concentration of Vinflunine can be increased when it is combined with Ranolazine.
Metreleptin The metabolism of Vinflunine can be increased when combined with Metreleptin.
Posaconazole The metabolism of Vinflunine can be decreased when combined with Posaconazole.
Voriconazole The metabolism of Vinflunine can be decreased when combined with Voriconazole.
Lopinavir The serum concentration of Vinflunine can be increased when it is combined with Lopinavir.
Crizotinib The metabolism of Vinflunine can be decreased when combined with Crizotinib.
Josamycin The serum concentration of Vinflunine can be increased when it is combined with Josamycin.
Tylvalosin The serum concentration of Vinflunine can be increased when it is combined with Tylvalosin.
Clindamycin The serum concentration of Vinflunine can be increased when it is combined with Clindamycin.
Mepartricin The serum concentration of Vinflunine can be increased when it is combined with Mepartricin.
Tilmicosin The serum concentration of Vinflunine can be increased when it is combined with Tilmicosin.
Tylosin The serum concentration of Vinflunine can be increased when it is combined with Tylosin.
Lumacaftor The serum concentration of Vinflunine can be decreased when it is combined with Lumacaftor.
Mitomycin The risk or severity of bronchospasm, shortness of breath, and dyspnea can be increased when Vinflunine is combined with Mitomycin.
Vemurafenib The serum concentration of Vinflunine can be increased when it is combined with Vemurafenib.
Apalutamide The serum concentration of Vinflunine can be decreased when it is combined with Apalutamide.
Pitolisant The serum concentration of Vinflunine can be decreased when it is combined with Pitolisant.
Isavuconazole The serum concentration of Vinflunine can be increased when it is combined with Isavuconazole.
Isavuconazonium The serum concentration of Vinflunine can be increased when it is combined with Isavuconazonium.
Levothyroxine The serum concentration of Vinflunine can be decreased when it is combined with Levothyroxine.
Trazodone The serum concentration of Vinflunine can be decreased when it is combined with Trazodone.
Dexamethasone acetate The serum concentration of Vinflunine can be decreased when it is combined with Dexamethasone acetate.
Reserpine The serum concentration of Vinflunine can be increased when it is combined with Reserpine.
Loxapine The serum concentration of Vinflunine can be increased when it is combined with Loxapine.
Toremifene The serum concentration of Vinflunine can be increased when it is combined with Toremifene.
Zonisamide The serum concentration of Vinflunine can be increased when it is combined with Zonisamide.
Carvedilol The serum concentration of Vinflunine can be increased when it is combined with Carvedilol.
Propafenone The serum concentration of Vinflunine can be increased when it is combined with Propafenone.
Paliperidone The serum concentration of Vinflunine can be increased when it is combined with Paliperidone.
Biricodar The serum concentration of Vinflunine can be increased when it is combined with Biricodar.
Elacridar The serum concentration of Vinflunine can be increased when it is combined with Elacridar.
Flibanserin The serum concentration of Vinflunine can be increased when it is combined with Flibanserin.
Vandetanib The serum concentration of Vinflunine can be increased when it is combined with Vandetanib.
Zosuquidar The serum concentration of Vinflunine can be increased when it is combined with Zosuquidar.
Tariquidar The serum concentration of Vinflunine can be increased when it is combined with Tariquidar.
Ponatinib The serum concentration of Vinflunine can be increased when it is combined with Ponatinib.
Canagliflozin The serum concentration of Vinflunine can be increased when it is combined with Canagliflozin.
Afatinib The serum concentration of Vinflunine can be increased when it is combined with Afatinib.
Ledipasvir The serum concentration of Vinflunine can be increased when it is combined with Ledipasvir.
Vorapaxar The serum concentration of Vinflunine can be increased when it is combined with Vorapaxar.
Suvorexant The serum concentration of Vinflunine can be increased when it is combined with Suvorexant.
Daclatasvir The serum concentration of Vinflunine can be increased when it is combined with Daclatasvir.
Niguldipine The serum concentration of Vinflunine can be increased when it is combined with Niguldipine.
Rolapitant The serum concentration of Vinflunine can be increased when it is combined with Rolapitant.
Velpatasvir The serum concentration of Vinflunine can be increased when it is combined with Velpatasvir.
Neratinib The serum concentration of Vinflunine can be increased when it is combined with Neratinib.
Valspodar The serum concentration of Vinflunine can be increased when it is combined with Valspodar.
Dacomitinib The serum concentration of Vinflunine can be increased when it is combined with Dacomitinib.
Glasdegib The serum concentration of Vinflunine can be increased when it is combined with Glasdegib.
Voxilaprevir The serum concentration of Vinflunine can be increased when it is combined with Voxilaprevir.
Sarecycline The serum concentration of Vinflunine can be increased when it is combined with Sarecycline.
Laniquidar The serum concentration of Vinflunine can be increased when it is combined with Laniquidar.
Pibrentasvir The serum concentration of Vinflunine can be increased when it is combined with Pibrentasvir.
Dexniguldipine The serum concentration of Vinflunine can be increased when it is combined with Dexniguldipine.
ONT-093 The serum concentration of Vinflunine can be increased when it is combined with ONT-093.
Mirabegron The serum concentration of Vinflunine can be increased when it is combined with Mirabegron.
Elagolix The serum concentration of Vinflunine can be increased when it is combined with Elagolix.
Sildenafil The serum concentration of Vinflunine can be increased when it is combined with Sildenafil.
Simvastatin The serum concentration of Vinflunine can be increased when it is combined with Simvastatin.
Vardenafil The serum concentration of Vinflunine can be increased when it is combined with Vardenafil.
Temsirolimus The serum concentration of Vinflunine can be increased when it is combined with Temsirolimus.
Entrectinib The serum concentration of Vinflunine can be increased when it is combined with Entrectinib.
Fedratinib The serum concentration of Vinflunine can be increased when it is combined with Fedratinib.
Istradefylline The serum concentration of Vinflunine can be increased when it is combined with Istradefylline.
Carfilzomib The serum concentration of Vinflunine can be increased when it is combined with Carfilzomib.
Everolimus The serum concentration of Vinflunine can be increased when it is combined with Everolimus.
Favipiravir The serum concentration of Vinflunine can be increased when it is combined with Favipiravir.
Ixabepilone The serum concentration of Vinflunine can be increased when it is combined with Ixabepilone.
Ripretinib The serum concentration of Vinflunine can be increased when it is combined with Ripretinib.
Pralsetinib The serum concentration of Vinflunine can be increased when it is combined with Pralsetinib.
Arsenic trioxide The serum concentration of Vinflunine can be increased when it is combined with Arsenic trioxide.
Mefloquine The serum concentration of Vinflunine can be increased when it is combined with Mefloquine.
Sorafenib The serum concentration of Vinflunine can be increased when it is combined with Sorafenib.
Eliglustat The serum concentration of Vinflunine can be increased when it is combined with Eliglustat.
Umbralisib The serum concentration of Vinflunine can be increased when it is combined with Umbralisib.
Diosmin The serum concentration of Vinflunine can be increased when it is combined with Diosmin.
Sapropterin The serum concentration of Vinflunine can be increased when it is combined with Sapropterin.
Regorafenib The serum concentration of Vinflunine can be increased when it is combined with Regorafenib.
Levoketoconazole The metabolism of Vinflunine can be decreased when combined with Levoketoconazole.
Belumosudil The serum concentration of Vinflunine can be increased when it is combined with Belumosudil.
Bexarotene The metabolism of Vinflunine can be increased when combined with Bexarotene.
Bosentan The metabolism of Vinflunine can be increased when combined with Bosentan.
Nafcillin The metabolism of Vinflunine can be increased when combined with Nafcillin.
Etravirine The metabolism of Vinflunine can be increased when combined with Etravirine.
Avasimibe The metabolism of Vinflunine can be increased when combined with Avasimibe.
Echinacea The metabolism of Vinflunine can be increased when combined with Echinacea.
Asunaprevir The serum concentration of Vinflunine can be increased when it is combined with Asunaprevir.
Topiramate The metabolism of Vinflunine can be increased when combined with Topiramate.
Rifabutin The metabolism of Vinflunine can be increased when combined with Rifabutin.
Warfarin The metabolism of Vinflunine can be increased when combined with Warfarin.
Felbamate The metabolism of Vinflunine can be increased when combined with Felbamate.
Genistein The metabolism of Vinflunine can be increased when combined with Genistein.
Oritavancin The metabolism of Vinflunine can be increased when combined with Oritavancin.
Rufinamide The metabolism of Vinflunine can be increased when combined with Rufinamide.
Glycerol phenylbutyrate The metabolism of Vinflunine can be increased when combined with Glycerol phenylbutyrate.
Eslicarbazepine acetate The metabolism of Vinflunine can be increased when combined with Eslicarbazepine acetate.
Lesinurad The metabolism of Vinflunine can be increased when combined with Lesinurad.
Sarilumab The metabolism of Vinflunine can be increased when combined with Sarilumab.

Target Protein

Tubulin beta chain TUBB

Referensi & Sumber

Synthesis reference: Fahy J, Hellier P, Breillout F, Bailly C. Vinflunine: discovery and synthesis of a novel microtubule inhibitor. Semin Oncol. 2008;35(3 Suppl 3):S3-5.
Artikel (PubMed)
  • PMID: 9515574
    Kruczynski A, Barret JM, Etievant C, Colpaert F, Fahy J, Hill BT: Antimitotic and tubulin-interacting properties of vinflunine, a novel fluorinated Vinca alkaloid. Biochem Pharmacol. 1998 Mar 1;55(5):635-48.
  • PMID: 11016627
    Ngan VK, Bellman K, Panda D, Hill BT, Jordan MA, Wilson L: Novel actions of the antitumor drugs vinflunine and vinorelbine on microtubules. Cancer Res. 2000 Sep 15;60(18):5045-51.
  • PMID: 28042310
    Gerullis H, Wawroschek F, Kohne CH, Ecke TH: Vinflunine in the treatment of advanced urothelial cancer: clinical evidence and experience. Ther Adv Urol. 2017 Jan;9(1):28-35. doi: 10.1177/1756287216677903. Epub 2016 Nov 21.
  • PMID: 18538179
    Jordan MA, Horwitz SB, Lobert S, Correia JJ: Exploring the mechanisms of action of the novel microtubule inhibitor vinflunine. Semin Oncol. 2008 Jun;35(3 Suppl 3):S6-S12. doi: 10.1053/j.seminoncol.2008.01.009.
  • PMID: 11408618
    Ngan VK, Bellman K, Hill BT, Wilson L, Jordan MA: Mechanism of mitotic block and inhibition of cell proliferation by the semisynthetic Vinca alkaloids vinorelbine and its newer derivative vinflunine. Mol Pharmacol. 2001 Jul;60(1):225-32.

Contoh Produk & Brand

Produk: 12 • International brands: 0
Produk
  • Javlor
    Injection, solution, concentrate • 25 mg/ml • Intravenous • EU • Approved
  • Javlor
    Injection, solution, concentrate • 25 mg/ml • Intravenous • EU • Approved
  • Javlor
    Injection, solution, concentrate • 25 mg/ml • Intravenous • EU • Approved
  • Javlor
    Injection, solution, concentrate • 25 mg/ml • Intravenous • EU • Approved
  • Javlor
    Injection, solution, concentrate • 25 mg/ml • Intravenous • EU • Approved
  • Javlor
    Injection, solution, concentrate • 25 mg/ml • Intravenous • EU • Approved
  • Javlor
    Injection, solution, concentrate • 25 mg/ml • Intravenous • EU • Approved
  • Javlor
    Injection, solution, concentrate • 25 mg/ml • Intravenous • EU • Approved
Menampilkan 8 dari 12 produk.

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