There is no known antidote for lusutrombopag: hemodialysis is not expected to enhance the elimination of lusutrombopag from the plasma as there is high protein binding. Overdose may be characterized by excessive platelet counts that may result in thrombotic and thromboembolic complications. In the event of overdose, closely monitor patients and platelet count and treat thrombotic complications in accordance with standard of care FDA Label.
In animal and in vitro studies, lusutrombopag did not display any carcinogenicity, genotoxicity, or reproductive toxicity FDA Label.
Lusutrombopag is an orally bioavailable thrombopoietin receptor (TPOR) agonist developed by Shionogi & Company (Osaka, Japan). TPOR is a regulatory target site for endogenous thrombopoietin, which acts as a primary cytokine to promote megakaryocyte proliferation and differentiation, and affect other hematopoietic lineages as well, including erythroid, granulocytic and lymphoid lineages A36736. Thrombocytopenia, which indicates abnormally low levels of platelets, is a common complication related to chronic liver disease. This hematological abnormality, especially in cases of severe thrombocytopenia (platelet count <50,000/?L), creates challenges to patients requiring invasive medical procedures where there is a significant risk for spontaneous bleeding A36732. Lusutrombopag binds to the transmembrane domain of TPOR expressed on megakaryocytes, and causes the proliferation and differentiation of megakaryocytic progenitor cells from hematopoietic stem cells FDA Label.
In September 2015, lusutrombopag received its first global approval in Japan to reduce the need for platelet transfusion in adults with chronic liver disease and thrombocytopenia who are schedule to undergo an invasive medical procedure A36730. Lusutrombopag was approved by the FDA on July 31st, 2018 for the same therapeutic indication under the market name Mulpleta. In two randomized, double-blind, placebo-controlled trials, patients with chronic liver disease and severe thrombocytopenia who were undergoing an invasive procedure with a platelet count less than 50 x 10^9/L were administered lusutrombopag orally L4166. Higher percentages (65-78%) of the patients receiving lusutrombopag required no platelet transfusion prior to the primary invasive procedure compared to those receiving placebo L4166. Lusutrombopag is currently in phase III development in various European countries including Austria, Belgium, Germany, and the UK A36730.
Fitur visualisasi ini dikembangkan menggunakan pendekatan Graph Theory untuk memetakan hubungan polifarmasi dan molekuler. Entitas (Obat, Target, Gen) direpresentasikan sebagai Simpul (Nodes), sedangkan hubungan biologisnya sebagai Sisi (Edges).
drugbank-id dan name pada skema XML DrugBank.targets/target yang memuat polipeptida sasaran.gene-name dan varian snp-effects.Tata letak grafik menggunakan algoritma Force-Directed Graph (Barnes-Hut). Model fisika ini menerapkan gaya tolak-menolak antar simpul (Gravitasi: -3000) agar tidak tumpang tindih, serta gaya pegas (Spring: 0.04) pada garis penghubung untuk fleksibilitas interaksi.
| Ranolazine | The serum concentration of Lusutrombopag can be increased when it is combined with Ranolazine. |
| Lumacaftor | The serum concentration of Lusutrombopag can be decreased when it is combined with Lumacaftor. |
| Vemurafenib | The serum concentration of Lusutrombopag can be increased when it is combined with Vemurafenib. |
| Apalutamide | The serum concentration of Lusutrombopag can be decreased when it is combined with Apalutamide. |
| Pitolisant | The serum concentration of Lusutrombopag can be increased when it is combined with Pitolisant. |
| Isavuconazole | The serum concentration of Lusutrombopag can be increased when it is combined with Isavuconazole. |
| Isavuconazonium | The serum concentration of Lusutrombopag can be increased when it is combined with Isavuconazonium. |
| Sulfasalazine | Sulfasalazine may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Novobiocin | Novobiocin may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Hesperetin | Hesperetin may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Rabeprazole | Rabeprazole may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Topiroxostat | Topiroxostat may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Daidzin | Daidzin may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Fusidic acid | Fusidic acid may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Naringenin | Naringenin may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Vandetanib | Vandetanib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Eltrombopag | Eltrombopag may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Safinamide | Safinamide may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Teriflunomide | Teriflunomide may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Cannabidiol | Cannabidiol may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Palbociclib | Palbociclib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Dacomitinib | Dacomitinib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Glasdegib | Glasdegib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Fostamatinib | Fostamatinib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Gilteritinib | Gilteritinib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Brigatinib | Brigatinib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Nabiximols | Nabiximols may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Fedratinib | Fedratinib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Istradefylline | Istradefylline may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Caffeine | Caffeine may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Pantoprazole | Pantoprazole may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Nelfinavir | Nelfinavir may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Diethylstilbestrol | Diethylstilbestrol may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Gefitinib | Gefitinib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Beclomethasone dipropionate | Beclomethasone dipropionate may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Progesterone | Progesterone may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Lansoprazole | Lansoprazole may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Imatinib | Imatinib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Estradiol | Estradiol may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Buprenorphine | Buprenorphine may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Telmisartan | Telmisartan may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Dexamethasone | Dexamethasone may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Sunitinib | Sunitinib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Genistein | Genistein may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Quercetin | Quercetin may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Vismodegib | Vismodegib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Rilpivirine | Rilpivirine may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Afatinib | Afatinib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Alectinib | Alectinib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Abemaciclib | Abemaciclib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Estradiol acetate | Estradiol acetate may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Estradiol benzoate | Estradiol benzoate may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Estradiol cypionate | Estradiol cypionate may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Estradiol dienanthate | Estradiol dienanthate may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Estradiol valerate | Estradiol valerate may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Cyclosporine | Cyclosporine may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Pravastatin | Pravastatin may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Erlotinib | Erlotinib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Dasatinib | Dasatinib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Taurocholic acid | Taurocholic acid may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Dovitinib | Dovitinib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Dabrafenib | Dabrafenib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Dasabuvir | Dasabuvir may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Paritaprevir | Paritaprevir may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Ripretinib | Ripretinib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Fostemsavir | Fostemsavir may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Pralsetinib | Pralsetinib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Clofazimine | Clofazimine may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Dexamethasone acetate | Dexamethasone acetate may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Avanafil | Avanafil may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Tivozanib | Tivozanib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Belumosudil | Belumosudil may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Fluconazole | The serum concentration of Lusutrombopag can be increased when it is combined with Fluconazole. |
| Erythromycin | The serum concentration of Lusutrombopag can be increased when it is combined with Erythromycin. |
| Sildenafil | The serum concentration of Lusutrombopag can be increased when it is combined with Sildenafil. |
| Reserpine | The serum concentration of Lusutrombopag can be increased when it is combined with Reserpine. |
| Sorafenib | The serum concentration of Lusutrombopag can be increased when it is combined with Sorafenib. |
| Loxapine | The serum concentration of Lusutrombopag can be increased when it is combined with Loxapine. |
| Quinine | The serum concentration of Lusutrombopag can be increased when it is combined with Quinine. |
| Ritonavir | Ritonavir may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Toremifene | The serum concentration of Lusutrombopag can be increased when it is combined with Toremifene. |
| Simvastatin | The serum concentration of Lusutrombopag can be increased when it is combined with Simvastatin. |
| Verapamil | The serum concentration of Lusutrombopag can be increased when it is combined with Verapamil. |
| Tamoxifen | The serum concentration of Lusutrombopag can be increased when it is combined with Tamoxifen. |
| Mifepristone | The serum concentration of Lusutrombopag can be increased when it is combined with Mifepristone. |
| Vardenafil | The serum concentration of Lusutrombopag can be increased when it is combined with Vardenafil. |
| Conivaptan | The serum concentration of Lusutrombopag can be increased when it is combined with Conivaptan. |
| Zonisamide | The serum concentration of Lusutrombopag can be increased when it is combined with Zonisamide. |
| Tipranavir | The serum concentration of Lusutrombopag can be increased when it is combined with Tipranavir. |
| Ketoconazole | The serum concentration of Lusutrombopag can be increased when it is combined with Ketoconazole. |
| Amiodarone | The serum concentration of Lusutrombopag can be increased when it is combined with Amiodarone. |
| Carvedilol | The serum concentration of Lusutrombopag can be increased when it is combined with Carvedilol. |
| Itraconazole | Itraconazole may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Propafenone | The serum concentration of Lusutrombopag can be increased when it is combined with Propafenone. |
| Clarithromycin | The serum concentration of Lusutrombopag can be increased when it is combined with Clarithromycin. |
| Saquinavir | Saquinavir may decrease the excretion rate of Lusutrombopag which could result in a higher serum level. |
| Lapatinib | The serum concentration of Lusutrombopag can be increased when it is combined with Lapatinib. |
| Paliperidone | The serum concentration of Lusutrombopag can be increased when it is combined with Paliperidone. |
| Mibefradil | The serum concentration of Lusutrombopag can be increased when it is combined with Mibefradil. |
| Lopinavir | The serum concentration of Lusutrombopag can be increased when it is combined with Lopinavir. |