Peringatan Keamanan

LD50 information for loncastuximab tesirine is not readily available in the literature. Toxicity is increased at higher doses, and may lead to discontinuation.A234459,L33559

Loncastuximab tesirine

DB16222

biotech approved investigational

Deskripsi

Relapsed and refractory B-cell acute lymphoblastic leukemia (B-ALL) are a therapeutic challenge for patients who have undergone prior systemic therapies with limited success.A234439 Prognosis is poor and more effective therapies are needed to treat relapsed/refractory cases and improve survival.A234444 On April 23 2021, the Food and Drug Administration granted accelerated approval for the antibody-drug conjugate, loncastuximab tesirine-lpyl, also known as Zynlonta. Zylonta also received approval in the EU on December 22, 2022.L45206 This therapy was developed by ADC Therapeutics and its accelerated approval for relapsed or refractory B-cell lymphoma is based on promising results from the LOTIS-2 clinical trial.L33559,L33634

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of loncastuximab tesirine-lpyl was 7.06-12.5 days at steady-state.[A234459,L33559]
Volume Distribusi In clinical studies, the average loncastuximab tesirine-lpyl volume of distribution was 7.11 liters, with a range between 7.19-8.43 liters.[A234459,L33559]
Klirens (Clearance) In pharmacokinetic studies, the mean clearance of loncastuximab tesirine-lpyl decreased with time from 0.499 L/day after a single dose to 0.275 L/day at steady-state.[L33559] One pharmacokinetic study measured a clearance ranging from 0.5-0.64 L/day.[A234459]

Absorpsi

Due to its intravenous route of administration, loncastuximab tesirine is readily absorbed into the circulation.L33559 Cmax during Cycle 1 of therapy was 2995 ?g/L and 3155 ?g/L in Cycle 2. AUC was 15,245 - 22,823 ?g*day/L during pharmacokinetic studies.A234459

Metabolisme

The monoclonal antibody portion of loncastuximab tesirine-lpyl is catabolized into small peptides. In vitro studies show that the small molecule cytotoxin portion, SG3199, is metabolized by CYP3A4/5.L33559

Rute Eliminasi

The main excretion pathways of SG3199 have not been formally studied in humans. SG3199 is thought to be minimally excreted by the kidneys.L33559

Interaksi Obat

644 Data
Ranolazine The serum concentration of Loncastuximab tesirine can be increased when it is combined with Ranolazine.
Lumacaftor The serum concentration of Loncastuximab tesirine can be decreased when it is combined with Lumacaftor.
Vemurafenib The serum concentration of Loncastuximab tesirine can be increased when it is combined with Vemurafenib.
Apalutamide The serum concentration of Loncastuximab tesirine can be decreased when it is combined with Apalutamide.
Pitolisant The serum concentration of Loncastuximab tesirine can be increased when it is combined with Pitolisant.
Isavuconazonium The serum concentration of Loncastuximab tesirine can be increased when it is combined with Isavuconazonium.
Isavuconazole The serum concentration of Loncastuximab tesirine can be increased when it is combined with Isavuconazole.
Cyclosporine The serum concentration of Loncastuximab tesirine can be increased when it is combined with Cyclosporine.
Fluconazole The serum concentration of Loncastuximab tesirine can be increased when it is combined with Fluconazole.
Erythromycin The serum concentration of Loncastuximab tesirine can be increased when it is combined with Erythromycin.
Sildenafil The serum concentration of Loncastuximab tesirine can be increased when it is combined with Sildenafil.
Reserpine The serum concentration of Loncastuximab tesirine can be increased when it is combined with Reserpine.
Mefloquine The serum concentration of Loncastuximab tesirine can be increased when it is combined with Mefloquine.
Sapropterin The serum concentration of Loncastuximab tesirine can be increased when it is combined with Sapropterin.
Sorafenib The serum concentration of Loncastuximab tesirine can be increased when it is combined with Sorafenib.
Loxapine The serum concentration of Loncastuximab tesirine can be increased when it is combined with Loxapine.
Quinine The serum concentration of Loncastuximab tesirine can be increased when it is combined with Quinine.
Ritonavir The serum concentration of Loncastuximab tesirine can be increased when it is combined with Ritonavir.
Toremifene The serum concentration of Loncastuximab tesirine can be increased when it is combined with Toremifene.
Simvastatin The serum concentration of Loncastuximab tesirine can be increased when it is combined with Simvastatin.
Verapamil The serum concentration of Loncastuximab tesirine can be increased when it is combined with Verapamil.
Tamoxifen The serum concentration of Loncastuximab tesirine can be increased when it is combined with Tamoxifen.
Mifepristone The serum concentration of Loncastuximab tesirine can be increased when it is combined with Mifepristone.
Clofazimine The serum concentration of Loncastuximab tesirine can be increased when it is combined with Clofazimine.
Vardenafil The serum concentration of Loncastuximab tesirine can be increased when it is combined with Vardenafil.
Tacrolimus The serum concentration of Loncastuximab tesirine can be increased when it is combined with Tacrolimus.
Conivaptan The serum concentration of Loncastuximab tesirine can be increased when it is combined with Conivaptan.
Quinidine The serum concentration of Loncastuximab tesirine can be increased when it is combined with Quinidine.
Zonisamide The serum concentration of Loncastuximab tesirine can be increased when it is combined with Zonisamide.
Tipranavir The serum concentration of Loncastuximab tesirine can be increased when it is combined with Tipranavir.
Norgestimate The serum concentration of Loncastuximab tesirine can be increased when it is combined with Norgestimate.
Ketoconazole The serum concentration of Loncastuximab tesirine can be increased when it is combined with Ketoconazole.
Amiodarone The serum concentration of Loncastuximab tesirine can be increased when it is combined with Amiodarone.
Carvedilol The serum concentration of Loncastuximab tesirine can be increased when it is combined with Carvedilol.
Itraconazole The serum concentration of Loncastuximab tesirine can be increased when it is combined with Itraconazole.
Arsenic trioxide The serum concentration of Loncastuximab tesirine can be increased when it is combined with Arsenic trioxide.
Propafenone The serum concentration of Loncastuximab tesirine can be increased when it is combined with Propafenone.
Clarithromycin The serum concentration of Loncastuximab tesirine can be increased when it is combined with Clarithromycin.
Saquinavir The serum concentration of Loncastuximab tesirine can be increased when it is combined with Saquinavir.
Lapatinib The serum concentration of Loncastuximab tesirine can be increased when it is combined with Lapatinib.
Paliperidone The serum concentration of Loncastuximab tesirine can be increased when it is combined with Paliperidone.
Mibefradil The serum concentration of Loncastuximab tesirine can be increased when it is combined with Mibefradil.
Everolimus The serum concentration of Loncastuximab tesirine can be increased when it is combined with Everolimus.
Lopinavir The serum concentration of Loncastuximab tesirine can be increased when it is combined with Lopinavir.
Ixabepilone The serum concentration of Loncastuximab tesirine can be increased when it is combined with Ixabepilone.
Biricodar The serum concentration of Loncastuximab tesirine can be increased when it is combined with Biricodar.
Dronedarone The serum concentration of Loncastuximab tesirine can be increased when it is combined with Dronedarone.
Nilotinib The serum concentration of Loncastuximab tesirine can be increased when it is combined with Nilotinib.
Elacridar The serum concentration of Loncastuximab tesirine can be increased when it is combined with Elacridar.
Flibanserin The serum concentration of Loncastuximab tesirine can be increased when it is combined with Flibanserin.
Vandetanib The serum concentration of Loncastuximab tesirine can be increased when it is combined with Vandetanib.
Telaprevir The serum concentration of Loncastuximab tesirine can be increased when it is combined with Telaprevir.
Zosuquidar The serum concentration of Loncastuximab tesirine can be increased when it is combined with Zosuquidar.
Tariquidar The serum concentration of Loncastuximab tesirine can be increased when it is combined with Tariquidar.
Temsirolimus The serum concentration of Loncastuximab tesirine can be increased when it is combined with Temsirolimus.
Simeprevir The serum concentration of Loncastuximab tesirine can be increased when it is combined with Simeprevir.
Cethromycin The serum concentration of Loncastuximab tesirine can be increased when it is combined with Cethromycin.
Lonafarnib The serum concentration of Loncastuximab tesirine can be increased when it is combined with Lonafarnib.
Brefeldin A The serum concentration of Loncastuximab tesirine can be increased when it is combined with Brefeldin A.
Ticagrelor The serum concentration of Loncastuximab tesirine can be increased when it is combined with Ticagrelor.
Ivacaftor The serum concentration of Loncastuximab tesirine can be increased when it is combined with Ivacaftor.
Lomitapide The serum concentration of Loncastuximab tesirine can be increased when it is combined with Lomitapide.
Crizotinib The serum concentration of Loncastuximab tesirine can be increased when it is combined with Crizotinib.
Linagliptin The serum concentration of Loncastuximab tesirine can be increased when it is combined with Linagliptin.
Carfilzomib The serum concentration of Loncastuximab tesirine can be increased when it is combined with Carfilzomib.
Mirabegron The serum concentration of Loncastuximab tesirine can be increased when it is combined with Mirabegron.
Regorafenib The serum concentration of Loncastuximab tesirine can be increased when it is combined with Regorafenib.
Ponatinib The serum concentration of Loncastuximab tesirine can be increased when it is combined with Ponatinib.
Canagliflozin The serum concentration of Loncastuximab tesirine can be increased when it is combined with Canagliflozin.
Afatinib The serum concentration of Loncastuximab tesirine can be increased when it is combined with Afatinib.
Diosmin The serum concentration of Loncastuximab tesirine can be increased when it is combined with Diosmin.
Ledipasvir The serum concentration of Loncastuximab tesirine can be increased when it is combined with Ledipasvir.
Vorapaxar The serum concentration of Loncastuximab tesirine can be increased when it is combined with Vorapaxar.
Suvorexant The serum concentration of Loncastuximab tesirine can be increased when it is combined with Suvorexant.
Eliglustat The serum concentration of Loncastuximab tesirine can be increased when it is combined with Eliglustat.
Netupitant The serum concentration of Loncastuximab tesirine can be increased when it is combined with Netupitant.
Cobicistat The serum concentration of Loncastuximab tesirine can be increased when it is combined with Cobicistat.
Palbociclib The serum concentration of Loncastuximab tesirine can be increased when it is combined with Palbociclib.
Daclatasvir The serum concentration of Loncastuximab tesirine can be increased when it is combined with Daclatasvir.
Niguldipine The serum concentration of Loncastuximab tesirine can be increased when it is combined with Niguldipine.
Methylene blue The serum concentration of Loncastuximab tesirine can be increased when it is combined with Methylene blue.
Rolapitant The serum concentration of Loncastuximab tesirine can be increased when it is combined with Rolapitant.
Venetoclax The serum concentration of Loncastuximab tesirine can be increased when it is combined with Venetoclax.
Asunaprevir The serum concentration of Loncastuximab tesirine can be increased when it is combined with Asunaprevir.
Velpatasvir The serum concentration of Loncastuximab tesirine can be increased when it is combined with Velpatasvir.
Voclosporin The serum concentration of Loncastuximab tesirine can be increased when it is combined with Voclosporin.
Istradefylline The serum concentration of Loncastuximab tesirine can be increased when it is combined with Istradefylline.
Neratinib The serum concentration of Loncastuximab tesirine can be increased when it is combined with Neratinib.
Valspodar The serum concentration of Loncastuximab tesirine can be increased when it is combined with Valspodar.
Dacomitinib The serum concentration of Loncastuximab tesirine can be increased when it is combined with Dacomitinib.
Glasdegib The serum concentration of Loncastuximab tesirine can be increased when it is combined with Glasdegib.
Elagolix The serum concentration of Loncastuximab tesirine can be increased when it is combined with Elagolix.
Entrectinib The serum concentration of Loncastuximab tesirine can be increased when it is combined with Entrectinib.
Voxilaprevir The serum concentration of Loncastuximab tesirine can be increased when it is combined with Voxilaprevir.
Sarecycline The serum concentration of Loncastuximab tesirine can be increased when it is combined with Sarecycline.
Favipiravir The serum concentration of Loncastuximab tesirine can be increased when it is combined with Favipiravir.
Fedratinib The serum concentration of Loncastuximab tesirine can be increased when it is combined with Fedratinib.
Laniquidar The serum concentration of Loncastuximab tesirine can be increased when it is combined with Laniquidar.
Enasidenib The serum concentration of Loncastuximab tesirine can be increased when it is combined with Enasidenib.
Pibrentasvir The serum concentration of Loncastuximab tesirine can be increased when it is combined with Pibrentasvir.

Target Protein

B-lymphocyte antigen CD19 CD19

Referensi & Sumber

Artikel (PubMed)
  • PMID: 32012214
    Jain N, Stock W, Zeidan A, Atallah E, McCloskey J, Heffner L, Tomlinson B, Bhatnagar B, Feingold J, Ungar D, Chao G, Zhang X, Qin Y, Havenith K, Kantarjian H, Wieduwilt MJ: Loncastuximab tesirine, an anti-CD19 antibody-drug conjugate, in relapsed/refractory B-cell acute lymphoblastic leukemia. Blood Adv. 2020 Feb 11;4(3):449-457. doi: 10.1182/bloodadvances.2019000767.
  • PMID: 33211842
    Hamadani M, Radford J, Carlo-Stella C, Caimi PF, Reid EG, O'Connor OA, Feingold J, Ardeshna KM, Townsend WM, Solh M, Heffner LT, Ungar D, Wang L, Boni JP, Havenith K, Qin YG, Kahl B: Final Results of a Phase 1 Study of Loncastuximab Tesirine in Relapsed/Refractory B-Cell Non-Hodgkin Lymphoma. Blood. 2020 Nov 19. pii: 474210. doi: 10.1182/blood.2020007512.
  • PMID: 29298756
    Zammarchi F, Corbett S, Adams L, Tyrer PC, Kiakos K, Janghra N, Marafioti T, Britten CE, Havenith CEG, Chivers S, D'Hooge F, Williams DG, Tiberghien A, Howard PW, Hartley JA, van Berkel PH: ADCT-402, a PBD dimer-containing antibody drug conjugate targeting CD19-expressing malignancies. Blood. 2018 Mar 8;131(10):1094-1105. doi: 10.1182/blood-2017-10-813493. Epub 2018 Jan 3.
  • PMID: 31685491
    Kahl BS, Hamadani M, Radford J, Carlo-Stella C, Caimi P, Reid E, Feingold JM, Ardeshna KM, Solh M, Heffner LT, Ungar D, He S, Boni J, Havenith K, O'Connor OA: A Phase I Study of ADCT-402 (Loncastuximab Tesirine), a Novel Pyrrolobenzodiazepine-Based Antibody-Drug Conjugate, in Relapsed/Refractory B-Cell Non-Hodgkin Lymphoma. Clin Cancer Res. 2019 Dec 1;25(23):6986-6994. doi: 10.1158/1078-0432.CCR-19-0711. Epub 2019 Nov 4.

Contoh Produk & Brand

Produk: 2 • International brands: 1
Produk
  • Zynlonta
    Injection, powder, for solution • 10 mg • Intravenous • EU • Approved
  • Zynlonta
    Injection, powder, lyophilized, for solution • 10 mg/2mL • Intravenous • US • Approved
International Brands
  • Zynlonta

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