Peringatan Keamanan

Data regarding overdosage with lurbinectedin are not available. Symptoms of overdose are likely to be consistent with lurbinectedin's adverse effect profile.L14327

Lurbinectedin

DB12674

small molecule approved investigational

Deskripsi

Lurbinectedin is a DNA alkylating agent that has been investigated in the treatment of a variety of cancers, including mesothelioma,A214325 chronic lymphocytic leukemia (CLL),A214328 breast cancer,A214322 and small-cell lung cancer (SCLC).A214310 It is a derivative of the marine-derived agent ecteinascidin (trabectedin), an anticancer agent found in extracts of the tunicate Ecteinascidia turbinata, with the primary difference being the substitution of the tetrahydroisoquinoline with a tetrahydro ??carboline that results in increased antitumour activity of lurbinectedin as compared to its predecessor.A214331

On June 15, 2020, the FDA granted accelerated approval and orphan drug designation to lurbinectedin for the treatment of adult patients with metastatic SCLC who have experienced disease progression despite therapy with platinum-based agents.L14336 This accelerated approval is based on the rate and duration of therapeutic response observed in ongoing clinical trials and is contingent on the verification of these results in confirmatory trials.

Struktur Molekul 2D

Berat 784.88
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal half-life of lurbinectedin is 51 hours.[L14327]
Volume Distribusi The steady-state volume of distribution of lurbinectedin is 504 L.[L14327]
Klirens (Clearance) The total plasma clearance of lurbinectedin is approximately 11 L/h.[L14327]

Absorpsi

Following intravenous administration, the Cmax and AUC0-inf were 107 µg/L and 551 µg*h/L, respectively. No accumulation between dosing intervals (every 3 weeks) has been observed.L14327 No significant differences in absorption were found between special populations (e.g. based on age, sex, ethnicity, etc.), but lurbinectedin has not been studied in the setting of severe renal impairment or moderate/severe hepatic impairment.

Metabolisme

Lurbinectedin is metabolized primarily by CYP3A4 in vitro, though specific data regarding its biotransformation are lacking.L14327 An N-desmethylated metabolite has been identified in canine subjects.A214319

Rute Eliminasi

Approximately 89% of a given dose is recovered in the feces (<0.2% unchanged) and 6% in the urine (1% unchanged).L14327

Interaksi Obat

156 Data
Pitolisant The serum concentration of Lurbinectedin can be decreased when it is combined with Pitolisant.
Metreleptin The metabolism of Lurbinectedin can be increased when combined with Metreleptin.
Cenobamate The serum concentration of Lurbinectedin can be decreased when it is combined with Cenobamate.
Tucatinib The metabolism of Tucatinib can be decreased when combined with Lurbinectedin.
Bexarotene The serum concentration of Lurbinectedin can be decreased when it is combined with Bexarotene.
Bosentan The serum concentration of Lurbinectedin can be decreased when it is combined with Bosentan.
Nafcillin The serum concentration of Lurbinectedin can be decreased when it is combined with Nafcillin.
Efavirenz The serum concentration of Lurbinectedin can be decreased when it is combined with Efavirenz.
Modafinil The serum concentration of Lurbinectedin can be decreased when it is combined with Modafinil.
Etravirine The serum concentration of Lurbinectedin can be decreased when it is combined with Etravirine.
Avasimibe The serum concentration of Lurbinectedin can be decreased when it is combined with Avasimibe.
Echinacea The serum concentration of Lurbinectedin can be decreased when it is combined with Echinacea.
Dexamethasone acetate The serum concentration of Lurbinectedin can be decreased when it is combined with Dexamethasone acetate.
Cyclosporine The serum concentration of Lurbinectedin can be increased when it is combined with Cyclosporine.
Fluvoxamine The serum concentration of Lurbinectedin can be increased when it is combined with Fluvoxamine.
Fluconazole The serum concentration of Lurbinectedin can be increased when it is combined with Fluconazole.
Erythromycin The serum concentration of Lurbinectedin can be increased when it is combined with Erythromycin.
Ziprasidone The serum concentration of Lurbinectedin can be increased when it is combined with Ziprasidone.
Isradipine The serum concentration of Lurbinectedin can be increased when it is combined with Isradipine.
Diltiazem The serum concentration of Lurbinectedin can be increased when it is combined with Diltiazem.
Clozapine The serum concentration of Lurbinectedin can be increased when it is combined with Clozapine.
Haloperidol The serum concentration of Lurbinectedin can be increased when it is combined with Haloperidol.
Ciprofloxacin The serum concentration of Lurbinectedin can be increased when it is combined with Ciprofloxacin.
Nicardipine The serum concentration of Lurbinectedin can be increased when it is combined with Nicardipine.
Verapamil The serum concentration of Lurbinectedin can be increased when it is combined with Verapamil.
Aprepitant The serum concentration of Lurbinectedin can be increased when it is combined with Aprepitant.
Isoniazid The serum concentration of Lurbinectedin can be increased when it is combined with Isoniazid.
Tioconazole The serum concentration of Lurbinectedin can be increased when it is combined with Tioconazole.
Primaquine The serum concentration of Lurbinectedin can be increased when it is combined with Primaquine.
Miconazole The serum concentration of Lurbinectedin can be increased when it is combined with Miconazole.
Fusidic acid The serum concentration of Lurbinectedin can be increased when it is combined with Fusidic acid.
Zimelidine The serum concentration of Lurbinectedin can be increased when it is combined with Zimelidine.
Dronedarone The serum concentration of Lurbinectedin can be increased when it is combined with Dronedarone.
Milnacipran The serum concentration of Lurbinectedin can be increased when it is combined with Milnacipran.
Simeprevir The serum concentration of Lurbinectedin can be increased when it is combined with Simeprevir.
Isavuconazonium The serum concentration of Lurbinectedin can be increased when it is combined with Isavuconazonium.
Desvenlafaxine The serum concentration of Lurbinectedin can be increased when it is combined with Desvenlafaxine.
Nilvadipine The serum concentration of Lurbinectedin can be increased when it is combined with Nilvadipine.
Seproxetine The serum concentration of Lurbinectedin can be increased when it is combined with Seproxetine.
Linagliptin The serum concentration of Lurbinectedin can be increased when it is combined with Linagliptin.
Luliconazole The serum concentration of Lurbinectedin can be increased when it is combined with Luliconazole.
Indalpine The serum concentration of Lurbinectedin can be increased when it is combined with Indalpine.
Netupitant The serum concentration of Lurbinectedin can be increased when it is combined with Netupitant.
Barnidipine The serum concentration of Lurbinectedin can be increased when it is combined with Barnidipine.
Benidipine The serum concentration of Lurbinectedin can be increased when it is combined with Benidipine.
Venetoclax The serum concentration of Lurbinectedin can be increased when it is combined with Venetoclax.
Isavuconazole The serum concentration of Lurbinectedin can be increased when it is combined with Isavuconazole.
Fosnetupitant The serum concentration of Lurbinectedin can be increased when it is combined with Fosnetupitant.
Berotralstat The serum concentration of Lurbinectedin can be increased when it is combined with Berotralstat.
Abametapir The serum concentration of Lurbinectedin can be increased when it is combined with Abametapir.
Satralizumab The serum concentration of Lurbinectedin can be decreased when it is combined with Satralizumab.
Sotorasib The serum concentration of Lurbinectedin can be decreased when it is combined with Sotorasib.
Terfenadine The serum concentration of Lurbinectedin can be increased when it is combined with Terfenadine.
Ritonavir The serum concentration of Lurbinectedin can be increased when it is combined with Ritonavir.
Voriconazole The serum concentration of Lurbinectedin can be increased when it is combined with Voriconazole.
Ergotamine The serum concentration of Lurbinectedin can be increased when it is combined with Ergotamine.
Delavirdine The serum concentration of Lurbinectedin can be increased when it is combined with Delavirdine.
Methimazole The serum concentration of Lurbinectedin can be increased when it is combined with Methimazole.
Conivaptan The serum concentration of Lurbinectedin can be increased when it is combined with Conivaptan.
Tipranavir The serum concentration of Lurbinectedin can be increased when it is combined with Tipranavir.
Telithromycin The serum concentration of Lurbinectedin can be increased when it is combined with Telithromycin.
Ketoconazole The serum concentration of Lurbinectedin can be increased when it is combined with Ketoconazole.
Atazanavir The serum concentration of Lurbinectedin can be increased when it is combined with Atazanavir.
Econazole The serum concentration of Lurbinectedin can be increased when it is combined with Econazole.
Nefazodone The serum concentration of Lurbinectedin can be increased when it is combined with Nefazodone.
Itraconazole The serum concentration of Lurbinectedin can be increased when it is combined with Itraconazole.
Clarithromycin The serum concentration of Lurbinectedin can be increased when it is combined with Clarithromycin.
Saquinavir The serum concentration of Lurbinectedin can be increased when it is combined with Saquinavir.
Posaconazole The serum concentration of Lurbinectedin can be increased when it is combined with Posaconazole.
Darunavir The serum concentration of Lurbinectedin can be increased when it is combined with Darunavir.
Lopinavir The serum concentration of Lurbinectedin can be increased when it is combined with Lopinavir.
Ditiocarb The serum concentration of Lurbinectedin can be increased when it is combined with Ditiocarb.
Nilotinib The serum concentration of Lurbinectedin can be increased when it is combined with Nilotinib.
Telaprevir The serum concentration of Lurbinectedin can be increased when it is combined with Telaprevir.
Boceprevir The serum concentration of Lurbinectedin can be increased when it is combined with Boceprevir.
Elvitegravir The serum concentration of Lurbinectedin can be increased when it is combined with Elvitegravir.
Stiripentol The serum concentration of Lurbinectedin can be increased when it is combined with Stiripentol.
Curcumin The serum concentration of Lurbinectedin can be increased when it is combined with Curcumin.
Ribociclib The serum concentration of Lurbinectedin can be increased when it is combined with Ribociclib.
Danoprevir The serum concentration of Lurbinectedin can be increased when it is combined with Danoprevir.
Troleandomycin The serum concentration of Lurbinectedin can be increased when it is combined with Troleandomycin.
Danazol The serum concentration of Lurbinectedin can be increased when it is combined with Danazol.
Lonafarnib The serum concentration of Lurbinectedin can be increased when it is combined with Lonafarnib.
Nelfinavir The serum concentration of Lurbinectedin can be increased when it is combined with Nelfinavir.
Indinavir The serum concentration of Lurbinectedin can be increased when it is combined with Indinavir.
Amprenavir The serum concentration of Lurbinectedin can be increased when it is combined with Amprenavir.
Amiodarone The serum concentration of Lurbinectedin can be increased when it is combined with Amiodarone.
Phenytoin The serum concentration of Lurbinectedin can be decreased when it is combined with Phenytoin.
Pentobarbital The serum concentration of Lurbinectedin can be decreased when it is combined with Pentobarbital.
Carbamazepine The serum concentration of Lurbinectedin can be decreased when it is combined with Carbamazepine.
Mitotane The serum concentration of Lurbinectedin can be decreased when it is combined with Mitotane.
Primidone The serum concentration of Lurbinectedin can be decreased when it is combined with Primidone.
Rimexolone The serum concentration of Lurbinectedin can be decreased when it is combined with Rimexolone.
Rifampin The serum concentration of Lurbinectedin can be decreased when it is combined with Rifampicin.
Phenobarbital The serum concentration of Lurbinectedin can be decreased when it is combined with Phenobarbital.
Dexamethasone The serum concentration of Lurbinectedin can be decreased when it is combined with Dexamethasone.
Fosphenytoin The serum concentration of Lurbinectedin can be decreased when it is combined with Fosphenytoin.
St. John's Wort The serum concentration of Lurbinectedin can be decreased when it is combined with St. John's Wort.
Midostaurin The serum concentration of Lurbinectedin can be decreased when it is combined with Midostaurin.
Enzalutamide The serum concentration of Lurbinectedin can be decreased when it is combined with Enzalutamide.

Target Protein

DNA

Referensi & Sumber

Synthesis reference: He W, Zhang Z, Ma D: A Scalable Total Synthesis of the Antitumor Agents Et-743 and Lurbinectedin. Angew Chem Int Ed Engl. 2019 Mar 18;58(12):3972-3975. doi: 10.1002/anie.201900035. Epub 2019 Feb 14.
Artikel (PubMed)
  • PMID: 32184690
    Kauffmann-Guerrero D, Huber RM: Orphan Drugs in Development for the Treatment of Small-Cell Lung Cancer: Emerging Data on Lurbinectedin. Lung Cancer (Auckl). 2020 Mar 2;11:27-31. doi: 10.2147/LCTT.S239223. eCollection 2020.
  • PMID: 30831452
    Altares R, Marquez Del Pino FM, Benedit G, Guillen MJ, Cuevas C, Perez de la Cruz MA, Aviles P: Development of a new method for the quantitation of metabolites in the absence of chemically synthetized authentic standards. J Pharm Biomed Anal. 2019 May 30;169:70-74. doi: 10.1016/j.jpba.2019.01.027. Epub 2019 Feb 21.
  • PMID: 30269906
    Gourd E: Lurbinectedin for BRCA-mutated advanced breast cancer. Lancet Oncol. 2018 Nov;19(11):e582. doi: 10.1016/S1470-2045(18)30737-X. Epub 2018 Sep 27.
  • PMID: 32085891
    Metaxas Y, Fruh M, Eboulet EI, Grosso F, Pless M, Zucali PA, Ceresoli GL, Mark M, Schneider M, Maconi A, Perrino M, Biaggi-Rudolf C, Froesch P, Schmid S, Waibel C, Appenzeller C, Rauch D, von Moos R: Lurbinectedin as second- or third-line palliative therapy in malignant pleural mesothelioma: an international, multi-centre, single-arm, phase II trial (SAKK 17/16). Ann Oncol. 2020 Apr;31(4):495-500. doi: 10.1016/j.annonc.2019.12.009. Epub 2020 Jan 16.
  • PMID: 32055920
    Risnik D, Colado A, Podaza E, Almejun MB, Elias EE, Bezares RF, Fernandez-Grecco H, Seija N, Oppezzo P, Borge M, Gamberale R, Giordano M: Immunoregulatory effects of Lurbinectedin in chronic lymphocytic leukemia. Cancer Immunol Immunother. 2020 May;69(5):813-824. doi: 10.1007/s00262-020-02513-y. Epub 2020 Feb 13.
  • PMID: 31621891
    Jimenez PC, Wilke DV, Branco PC, Bauermeister A, Rezende-Teixeira P, Gaudencio SP, Costa-Lotufo LV: Enriching cancer pharmacology with drugs of marine origin. Br J Pharmacol. 2020 Jan;177(1):3-27. doi: 10.1111/bph.14876. Epub 2019 Dec 23.

Contoh Produk & Brand

Produk: 2 • International brands: 1
Produk
  • Zepzelca
    Injection, powder, lyophilized, for solution • .5 mg/1mL • Intravenous • US • Approved
  • Zepzelca
    Powder • 4 mg / vial • Intravenous • Canada • Approved
International Brands
  • Zepsyre

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