Peringatan Keamanan

There are no data regarding overdosage with belumosudil.

Belumosudil

DB16703

small molecule approved investigational

Deskripsi

Belumosudil is used in the treatment of chronic graft-versus-host disease (GVHD) and has been investigated for the treatment of pulmonary arterial hypertension.A236634 It is an inhibitor of rho-associated coiled-coil-containing protein kinases (ROCK), with significantly more selectivity for ROCK2 as compared to ROCK1 (IC50 100 nM vs. 3 ?M, respectively).L34749 In the treatment of GVHD, a condition in which donor T-cells begin to attack recipient tissues following allogeneic hematopoeitic stem cell transplantation (HSCT), belumosudil helps to resolve immune dysregulation by shifting the balance between Th17 cells and T-regulatory cells, thereby dampening the inflammatory cascade that can occasionally be fatal.A236644,L34759

Belumosudil was first approved by the FDA in July 2021, under the brand name Rezurock, for the treatment of chronic GVHD in patients who have tried and failed at least two prior lines of systemic therapy.L34754 In July 2022, Belumosudil was approved by Health Canada under the brand name RHOLISTIQ to treat the same condition in adult and pediatric patients 12 years or older.L42925

Struktur Molekul 2D

Berat 452.518
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 elimination half-life of belumosudil following oral administration is 19 hours.[L34749]
Volume Distribusi Following a single oral dose of belumosudil in healthy subjects, the mean geometric volume of distribution was 184 L.[L34749]
Klirens (Clearance) The mean clearance of belumosudil is 9.83 L/h.[L34749]

Absorpsi

Following oral administration, the mean bioavailability of belumosudil is 64% and the median Tmax at steady-state is 1.26 to 2.53 hours.L34749 As compared to administration in a fasted state, belumosudil Cmax and AUC increased by 2.2 and 2 times, respectively, when administered with a high-fat, high-calorie meal.L34749

Metabolisme

The in vitro metabolism of belumosudil occurs primarily via CYP3A4 and to a lesser extent by CYP2C8, CYP2D6, and UGT1A9.L34749 The specific metabolites generated by belumosudil metabolism remain unclear.

Rute Eliminasi

Belumosudil is eliminated primarily in the feces. Following the administration of a radiolabeled oral dose of belumosudil in healthy subjects, approximately 85% of the radioactivity was recovered in the feces, 30% of which was unchanged parent drug, with less than 5% recovered in the urine.L34749

Interaksi Makanan

2 Data
  • 1. Take at the same time every day. Belumosudil should be taken with a meal at approximately the same time each day.
  • 2. Take with food. The co-administration of food increases the absorption of belumosudil.

Interaksi Obat

643 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Belumosudil.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Belumosudil.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Belumosudil.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Belumosudil.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Belumosudil.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Belumosudil.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Belumosudil.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Belumosudil.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Belumosudil.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Belumosudil.
Silodosin The excretion of Silodosin can be decreased when combined with Belumosudil.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Belumosudil.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Belumosudil.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Belumosudil.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Belumosudil.
Vincristine The excretion of Vincristine can be decreased when combined with Belumosudil.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Belumosudil.
Betrixaban The serum concentration of Betrixaban can be increased when it is combined with Belumosudil.
Pitolisant The serum concentration of Belumosudil can be decreased when it is combined with Pitolisant.
Folic acid Belumosudil may decrease the excretion rate of Folic acid which could result in a higher serum level.
Pravastatin Belumosudil may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Cladribine The excretion of Cladribine can be decreased when combined with Belumosudil.
Conjugated estrogens Belumosudil may decrease the excretion rate of Conjugated estrogens which could result in a higher serum level.
Gefitinib Belumosudil may decrease the excretion rate of Gefitinib which could result in a higher serum level.
Sorafenib The risk or severity of adverse effects can be increased when Sorafenib is combined with Belumosudil.
Allopurinol Belumosudil may decrease the excretion rate of Allopurinol which could result in a higher serum level.
Cerivastatin Belumosudil may decrease the excretion rate of Cerivastatin which could result in a higher serum level.
Teniposide The risk or severity of adverse effects can be increased when Teniposide is combined with Belumosudil.
Prazosin Belumosudil may decrease the excretion rate of Prazosin which could result in a higher serum level.
Raloxifene Belumosudil may decrease the excretion rate of Raloxifene which could result in a higher serum level.
Celecoxib Belumosudil may decrease the excretion rate of Celecoxib which could result in a higher serum level.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Belumosudil.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Belumosudil.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Belumosudil.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Belumosudil.
Ivermectin Belumosudil may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Imatinib The risk or severity of adverse effects can be increased when Imatinib is combined with Belumosudil.
Testosterone Belumosudil may decrease the excretion rate of Testosterone which could result in a higher serum level.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Belumosudil.
Sumatriptan Belumosudil may decrease the excretion rate of Sumatriptan which could result in a higher serum level.
Tamoxifen Belumosudil may decrease the excretion rate of Tamoxifen which could result in a higher serum level.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Belumosudil.
Daunorubicin The risk or severity of adverse effects can be increased when Daunorubicin is combined with Belumosudil.
Nitrofurantoin Belumosudil may decrease the excretion rate of Nitrofurantoin which could result in a higher serum level.
Lamivudine Belumosudil may decrease the excretion rate of Lamivudine which could result in a higher serum level.
Riluzole Belumosudil may decrease the excretion rate of Riluzole which could result in a higher serum level.
Irinotecan The risk or severity of adverse effects can be increased when Irinotecan is combined with Belumosudil.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Belumosudil.
Donepezil Belumosudil may decrease the excretion rate of Donepezil which could result in a higher serum level.
Ezetimibe Belumosudil may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Glyburide Belumosudil may decrease the excretion rate of Glyburide which could result in a higher serum level.
Tegaserod Belumosudil may decrease the excretion rate of Tegaserod which could result in a higher serum level.
Leflunomide The risk or severity of adverse effects can be increased when Belumosudil is combined with Leflunomide.
Rosuvastatin Belumosudil may decrease the excretion rate of Rosuvastatin which could result in a higher serum level.
Mitoxantrone The risk or severity of adverse effects can be increased when Mitoxantrone is combined with Belumosudil.
Alvocidib Belumosudil may decrease the excretion rate of Alvocidib which could result in a higher serum level.
Camptothecin Belumosudil may decrease the excretion rate of Camptothecin which could result in a higher serum level.
Rivaroxaban Belumosudil may decrease the excretion rate of Rivaroxaban which could result in a higher serum level.
Simeprevir The metabolism of Belumosudil can be decreased when combined with Simeprevir.
Apixaban Belumosudil may decrease the excretion rate of Apixaban which could result in a higher serum level.
Pralatrexate The risk or severity of adverse effects can be increased when Pralatrexate is combined with Belumosudil.
Teriflunomide The risk or severity of adverse effects can be increased when Teriflunomide is combined with Belumosudil.
Ponatinib The risk or severity of adverse effects can be increased when Ponatinib is combined with Belumosudil.
Dolutegravir Belumosudil may decrease the excretion rate of Dolutegravir which could result in a higher serum level.
Riociguat Belumosudil may decrease the excretion rate of Riociguat which could result in a higher serum level.
Sofosbuvir Belumosudil may decrease the excretion rate of Sofosbuvir which could result in a higher serum level.
Idelalisib The risk or severity of adverse effects can be increased when Idelalisib is combined with Belumosudil.
Palbociclib The risk or severity of adverse effects can be increased when Palbociclib is combined with Belumosudil.
Lenvatinib Belumosudil may decrease the excretion rate of Lenvatinib which could result in a higher serum level.
Fimasartan Belumosudil may decrease the excretion rate of Fimasartan which could result in a higher serum level.
Ombitasvir Belumosudil may decrease the excretion rate of Ombitasvir which could result in a higher serum level.
Tenofovir alafenamide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Belumosudil.
Velpatasvir Belumosudil may decrease the excretion rate of Velpatasvir which could result in a higher serum level.
Selumetinib Belumosudil may decrease the excretion rate of Selumetinib which could result in a higher serum level.
Fostemsavir Belumosudil may decrease the excretion rate of Fostemsavir which could result in a higher serum level.
Delafloxacin Belumosudil may decrease the excretion rate of Delafloxacin which could result in a higher serum level.
Duvelisib Belumosudil may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Glasdegib Belumosudil may decrease the excretion rate of Glasdegib which could result in a higher serum level.
Voxilaprevir Belumosudil may decrease the excretion rate of Voxilaprevir which could result in a higher serum level.
Brigatinib Belumosudil may decrease the excretion rate of Brigatinib which could result in a higher serum level.
Rucaparib Belumosudil may decrease the excretion rate of Rucaparib which could result in a higher serum level.
Tazemetostat Belumosudil may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Darolutamide Belumosudil may decrease the excretion rate of Darolutamide which could result in a higher serum level.
Lusutrombopag Belumosudil may decrease the excretion rate of Lusutrombopag which could result in a higher serum level.
Enasidenib Belumosudil may decrease the excretion rate of Enasidenib which could result in a higher serum level.
Pibrentasvir Belumosudil may decrease the excretion rate of Pibrentasvir which could result in a higher serum level.
Glecaprevir Belumosudil may decrease the excretion rate of Glecaprevir which could result in a higher serum level.
Testosterone cypionate Belumosudil may decrease the excretion rate of Testosterone cypionate which could result in a higher serum level.
Testosterone enanthate Belumosudil may decrease the excretion rate of Testosterone enanthate which could result in a higher serum level.
Ripretinib Belumosudil may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Trilaciclib Belumosudil may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Daptomycin The serum concentration of Daptomycin can be increased when it is combined with Belumosudil.
Sildenafil The serum concentration of Sildenafil can be increased when it is combined with Belumosudil.
Morphine The serum concentration of Morphine can be increased when it is combined with Belumosudil.
Tenofovir disoproxil The serum concentration of Tenofovir disoproxil can be increased when it is combined with Belumosudil.
Clobazam The serum concentration of Clobazam can be increased when it is combined with Belumosudil.
Mefloquine The serum concentration of Mefloquine can be increased when it is combined with Belumosudil.
Quinine The serum concentration of Quinine can be increased when it is combined with Belumosudil.
Toremifene The serum concentration of Toremifene can be increased when it is combined with Belumosudil.
Bisoprolol The serum concentration of Bisoprolol can be increased when it is combined with Belumosudil.

Target Protein

Rho-associated protein kinase 2 ROCK2
Rho-associated protein kinase 1 ROCK1

Referensi & Sumber

Synthesis reference: ??, ???, ??, ???, ???, ???, ??, and ???. The Synthetic Method of SLx 2119. SHANGHAI SCIENPHARM BIOTECHNOLOGY Co.,Ltd., assignee. Patent CN106916145A. 4 June 2019.
Artikel (PubMed)
  • PMID: 34265047
    Cutler CS, Lee SJ, Arai S, Rotta M, Zoghi B, Lazaryan A, Ramakrishnan A, DeFilipp Z, Salhotra A, Chai-Ho W, Mehta RS, Wang T, Arora M, Pusic I, Saad A, Shah NN, Abhyankar S, Bachier C, Galvin JP, Im A, Langston A, Liesveld JL, Juckett M, Logan A, Schachter L, Alavi A, Howard DS, Waksal H, Ryan J, Eiznhamer D, Aggarwal SK, Ieyoub J, Schueller O, Green LS, Yang Z, Krenz H, Jagasia M, Blazar BR, Pavletic SZ: Belumosudil for Chronic Graft-versus-Host Disease (cGVHD) After 2 or More Prior Lines of Therapy: The ROCKstar Study. Blood. 2021 Jul 15. pii: 476399. doi: 10.1182/blood.2021012021.
  • PMID: 34095764
    Braun LM, Zeiser R: Immunomodulatory Therapies for the Treatment of Graft-versus-host Disease. Hemasphere. 2021 Jun 1;5(6):e581. doi: 10.1097/HS9.0000000000000581. eCollection 2021 Jun.
  • PMID: 16412784
    Ferrara JL, Reddy P: Pathophysiology of graft-versus-host disease. Semin Hematol. 2006 Jan;43(1):3-10. doi: 10.1053/j.seminhematol.2005.09.001.
  • PMID: 33160621
    Yamamura A, Nayeem MJ, Sato M: The Rho kinase 2 (ROCK2)-specific inhibitor KD025 ameliorates the development of pulmonary arterial hypertension. Biochem Biophys Res Commun. 2021 Jan 1;534:795-801. doi: 10.1016/j.bbrc.2020.10.106. Epub 2020 Nov 5.

Contoh Produk & Brand

Produk: 3 • International brands: 1
Produk
  • Rezurock
    Tablet • 200 mg/1 • Oral • US • Approved
  • Rezurock
    Tablet • 200 mg/1 • Oral • US • Approved
  • Rezurock
    Tablet • 200 mg • Oral • Canada • Approved
International Brands
  • Rezurock — Kadmon Holdings, Inc.

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