Peringatan Keamanan

No information is available regarding the LD50. There is no known antidote for overdose with momelotinib. If an overdose is suspected, the patient should be monitored for signs or symptoms of adverse reactions or effects, and appropriate supportive treatment should be instituted immediately. Further management should be as clinically indicated. Hemodialysis is not expected to enhance the elimination of momelotinib.L48186

Momelotinib

DB11763

small molecule approved investigational

Deskripsi

Momelotinib is a Janus Kinase 1 (JAK1) and 2 (JAK2) inhibitor. It is a competitive inhibitor of JAK ATP binding.A261566 First approved by the FDA on September 15, 2023,L48206 momelotinib is used to treat myelofibrosis.L48186 Myelofibrosis (MF) is a group of myeloproliferative neoplasms characterized by abnormal proliferative hematopoietic stem cells, leading to the release of cytokines and growth factors. MF includes primary MF (PMF), post-polycythemia vera (PV) MF, and post-essential thrombocythemia (ET) MF. Clinical manifestations of MF include anemia and thrombocytosis. Momelotinib works to block the JAK-signal transducer and activator of transcription (STAT) signalling pathway, which is aberrant in MF.A261561, A261566, A261571

Struktur Molekul 2D

Berat 414.469
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of momelotinib and the M21 metabolite is four to eight hours.[L48186]
Volume Distribusi The mean (%CV) apparent volume of distribution at steady-state is 984 L (118%).[L48186]
Klirens (Clearance) The mean (%CV) clearance is clearance is 103 L/h (87%).[L48186]

Absorpsi

Momelotinib is rapidly absorbed following oral administration with a bioavailability of 97%.A261561 The mean (%CV) steady-state Cmax is 479 ng/mL (61%), and the mean (%CV) AUC is 3,288 ng x h/mL (60%) at the maximum recommended dosage. Momelotinib exposure (i.e., Cmax and AUC) increases dose proportionally from 100 mg to 300 mg (0.5 to 1.5 times the maximum recommended dosage), but less than dose-proportional at doses from 400 mg to 800 mg (two to four times the maximum recommended dosage). There is no clinically significant accumulation. The Tmax at steady state is two hours (Q1: 1 hour; Q3: 3 hours) post-dose.L48186 No clinically significant differences in momelotinib pharmacokinetics were observed following administration of either a high-fat meal (800 kcal; 50% fat) or low-fat meal (400 kcal; 20% fat) in healthy subjects.L48186

Metabolisme

Momelotinib is metabolized by multiple cytochrome P450 (CYP) enzymes, including CYP3A4 (36%), CYP2C8 (19%), CYP2C9 (17%), CYP2C19 (19%), and CYP1A2 (9%). M21 is initially formed via oxidation of the morpholine ring by the same CYP enzymes, followed by metabolism via aldehyde oxidase.A261551, L48186 M21 is a major metabolite in humans that retains approximately 40% of the pharmacological activity of the parent. The mean ratio of M21 to momelotinib for AUC ranged from 1.4 to 2.1.L48186 Momelotinib can undergo amide hydrolysis, N-dealkylation, nitrile hydrolysis, nitrile oxidation, and glucuronidation.A261546

Rute Eliminasi

Momelotinib is primarily eliminated in feces and, to a lesser extent, in urine. Following a single oral dose of radiolabeled momelotinib in healthy subjects, about 69% of the total radioactive dose was recovered in fecesm with M14 accounting for 21.4% of the dose, momelotinib and M21 each accounting for 13%, and other 12 metabolites accounting for the remaining 22%. About 28% of radioactivity was recovered in urine, with M21 being the major species.A261551, L48186

Interaksi Makanan

1 Data
  • 1. Take with or without food. Food has no clinically significant effect on drug exposure.

Interaksi Obat

243 Data
Cholic Acid The serum concentration of Momelotinib can be increased when it is combined with Cholic Acid.
Taurocholic acid The serum concentration of Momelotinib can be increased when it is combined with Taurocholic acid.
Apalutamide The serum concentration of Momelotinib can be decreased when it is combined with Apalutamide.
Folic acid The serum concentration of Folic acid can be increased when it is combined with Momelotinib.
Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Momelotinib.
Conjugated estrogens The serum concentration of Conjugated estrogens can be increased when it is combined with Momelotinib.
Gefitinib The serum concentration of Gefitinib can be increased when it is combined with Momelotinib.
Allopurinol The serum concentration of Allopurinol can be increased when it is combined with Momelotinib.
Cerivastatin The serum concentration of Cerivastatin can be increased when it is combined with Momelotinib.
Teniposide The serum concentration of Teniposide can be increased when it is combined with Momelotinib.
Prazosin The serum concentration of Prazosin can be increased when it is combined with Momelotinib.
Raloxifene The serum concentration of Raloxifene can be increased when it is combined with Momelotinib.
Celecoxib The serum concentration of Celecoxib can be increased when it is combined with Momelotinib.
Zidovudine The serum concentration of Zidovudine can be increased when it is combined with Momelotinib.
Ritonavir The serum concentration of Ritonavir can be increased when it is combined with Momelotinib.
Oxaliplatin The serum concentration of Oxaliplatin can be increased when it is combined with Momelotinib.
Vincristine The serum concentration of Vincristine can be increased when it is combined with Momelotinib.
Fluorouracil The serum concentration of Fluorouracil can be increased when it is combined with Momelotinib.
Methotrexate The serum concentration of Methotrexate can be increased when it is combined with Momelotinib.
Ivermectin The serum concentration of Ivermectin can be increased when it is combined with Momelotinib.
Imatinib The serum concentration of Imatinib can be increased when it is combined with Momelotinib.
Testosterone The serum concentration of Testosterone can be increased when it is combined with Momelotinib.
Clofarabine The serum concentration of Clofarabine can be increased when it is combined with Momelotinib.
Sumatriptan The serum concentration of Sumatriptan can be increased when it is combined with Momelotinib.
Tamoxifen The serum concentration of Tamoxifen can be increased when it is combined with Momelotinib.
Mycophenolate mofetil The serum concentration of Mycophenolate mofetil can be increased when it is combined with Momelotinib.
Daunorubicin The serum concentration of Daunorubicin can be increased when it is combined with Momelotinib.
Nitrofurantoin The serum concentration of Nitrofurantoin can be increased when it is combined with Momelotinib.
Lamivudine The serum concentration of Lamivudine can be increased when it is combined with Momelotinib.
Riluzole The serum concentration of Riluzole can be increased when it is combined with Momelotinib.
Irinotecan The serum concentration of Irinotecan can be increased when it is combined with Momelotinib.
Etoposide The serum concentration of Etoposide can be increased when it is combined with Momelotinib.
Sulfasalazine The serum concentration of Sulfasalazine can be increased when it is combined with Momelotinib.
Donepezil The serum concentration of Donepezil can be increased when it is combined with Momelotinib.
Dactinomycin The serum concentration of Dactinomycin can be increased when it is combined with Momelotinib.
Ezetimibe The serum concentration of Ezetimibe can be increased when it is combined with Momelotinib.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Momelotinib.
Glyburide The serum concentration of Glyburide can be increased when it is combined with Momelotinib.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Momelotinib.
Tegaserod The serum concentration of Tegaserod can be increased when it is combined with Momelotinib.
Leflunomide The serum concentration of Leflunomide can be increased when it is combined with Momelotinib.
Rosuvastatin The serum concentration of Rosuvastatin can be increased when it is combined with Momelotinib.
Mitoxantrone The serum concentration of Mitoxantrone can be increased when it is combined with Momelotinib.
Dasatinib The serum concentration of Dasatinib can be increased when it is combined with Momelotinib.
Alvocidib The serum concentration of Alvocidib can be increased when it is combined with Momelotinib.
Camptothecin The serum concentration of Camptothecin can be increased when it is combined with Momelotinib.
Nilotinib The serum concentration of Nilotinib can be increased when it is combined with Momelotinib.
Rivaroxaban The serum concentration of Rivaroxaban can be increased when it is combined with Momelotinib.
Simeprevir The serum concentration of Simeprevir can be increased when it is combined with Momelotinib.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Momelotinib.
Apixaban The serum concentration of Apixaban can be increased when it is combined with Momelotinib.
Pralatrexate The serum concentration of Pralatrexate can be increased when it is combined with Momelotinib.
Teriflunomide The serum concentration of Teriflunomide can be increased when it is combined with Momelotinib.
Vemurafenib The serum concentration of Vemurafenib can be increased when it is combined with Momelotinib.
Ponatinib The serum concentration of Ponatinib can be increased when it is combined with Momelotinib.
Dabrafenib The serum concentration of Dabrafenib can be increased when it is combined with Momelotinib.
Afatinib The serum concentration of Afatinib can be increased when it is combined with Momelotinib.
Dolutegravir The serum concentration of Dolutegravir can be increased when it is combined with Momelotinib.
Riociguat The serum concentration of Riociguat can be increased when it is combined with Momelotinib.
Sofosbuvir The serum concentration of Sofosbuvir can be increased when it is combined with Momelotinib.
Idelalisib The serum concentration of Idelalisib can be increased when it is combined with Momelotinib.
Palbociclib The serum concentration of Palbociclib can be increased when it is combined with Momelotinib.
Lenvatinib The serum concentration of Lenvatinib can be increased when it is combined with Momelotinib.
Fimasartan The serum concentration of Fimasartan can be increased when it is combined with Momelotinib.
Ombitasvir The serum concentration of Ombitasvir can be increased when it is combined with Momelotinib.
Tenofovir alafenamide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Momelotinib.
Osimertinib The serum concentration of Osimertinib can be increased when it is combined with Momelotinib.
Venetoclax The serum concentration of Venetoclax can be increased when it is combined with Momelotinib.
Velpatasvir The serum concentration of Velpatasvir can be increased when it is combined with Momelotinib.
Tucatinib The serum concentration of Tucatinib can be increased when it is combined with Momelotinib.
Selumetinib The serum concentration of Selumetinib can be increased when it is combined with Momelotinib.
Talazoparib The serum concentration of Talazoparib can be increased when it is combined with Momelotinib.
Fostemsavir The serum concentration of Fostemsavir can be increased when it is combined with Momelotinib.
Revefenacin The serum concentration of Revefenacin can be increased when it is combined with Momelotinib.
Delafloxacin The serum concentration of Delafloxacin can be increased when it is combined with Momelotinib.
Duvelisib The serum concentration of Duvelisib can be increased when it is combined with Momelotinib.
Dacomitinib The serum concentration of Dacomitinib can be increased when it is combined with Momelotinib.
Glasdegib The serum concentration of Glasdegib can be increased when it is combined with Momelotinib.
Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Momelotinib.
Alpelisib The serum concentration of Alpelisib can be increased when it is combined with Momelotinib.
Voxilaprevir The serum concentration of Voxilaprevir can be increased when it is combined with Momelotinib.
Brigatinib The serum concentration of Brigatinib can be increased when it is combined with Momelotinib.
Rucaparib The serum concentration of Rucaparib can be increased when it is combined with Momelotinib.
Rimegepant The serum concentration of Rimegepant can be increased when it is combined with Momelotinib.
Copanlisib The serum concentration of Copanlisib can be increased when it is combined with Momelotinib.
Ozanimod Momelotinib may decrease the excretion rate of Ozanimod which could result in a higher serum level.
Tazemetostat The serum concentration of Tazemetostat can be increased when it is combined with Momelotinib.
Darolutamide The serum concentration of Darolutamide can be increased when it is combined with Momelotinib.
Lusutrombopag The serum concentration of Lusutrombopag can be increased when it is combined with Momelotinib.
Enasidenib The serum concentration of Enasidenib can be increased when it is combined with Momelotinib.
Pibrentasvir The serum concentration of Pibrentasvir can be increased when it is combined with Momelotinib.
Glecaprevir The serum concentration of Glecaprevir can be increased when it is combined with Momelotinib.
Testosterone cypionate The serum concentration of Testosterone cypionate can be increased when it is combined with Momelotinib.
Testosterone enanthate The serum concentration of Testosterone enanthate can be increased when it is combined with Momelotinib.
Ripretinib The serum concentration of Ripretinib can be increased when it is combined with Momelotinib.
Ubrogepant The serum concentration of Ubrogepant can be increased when it is combined with Momelotinib.
Trilaciclib The serum concentration of Trilaciclib can be increased when it is combined with Momelotinib.
Pralsetinib The serum concentration of Pralsetinib can be increased when it is combined with Momelotinib.
Berotralstat The serum concentration of Berotralstat can be increased when it is combined with Momelotinib.
Cyclosporine The serum concentration of Momelotinib can be increased when it is combined with Cyclosporine.

Target Protein

Tyrosine-protein kinase JAK1 JAK1
Tyrosine-protein kinase JAK2 JAK2
Tyrosine-protein kinase JAK3 JAK3
Non-receptor tyrosine-protein kinase TYK2 TYK2
Activin receptor type-1 ACVR1
Receptor-type tyrosine-protein kinase FLT3 FLT3

Referensi & Sumber

Artikel (PubMed)
  • PMID: 29311136
    Zheng J, Xin Y, Zhang J, Subramanian R, Murray BP, Whitney JA, Warr MR, Ling J, Moorehead L, Kwan E, Hemenway J, Smith BJ, Silverman JA: Pharmacokinetics and Disposition of Momelotinib Revealed a Disproportionate Human Metabolite-Resolution for Clinical Development. Drug Metab Dispos. 2018 Mar;46(3):237-247. doi: 10.1124/dmd.117.078899. Epub 2018 Jan 8.
  • PMID: 29283448
    Xin Y, Kawashima J, Weng W, Kwan E, Tarnowski T, Silverman JA: Pharmacokinetics and Safety of Momelotinib in Subjects With Hepatic or Renal Impairment. J Clin Pharmacol. 2018 Apr;58(4):522-532. doi: 10.1002/jcph.1050. Epub 2017 Dec 28.
  • PMID: 31450973
    Xu L, Feng J, Gao G, Tang H: Momelotinib for the treatment of myelofibrosis. Expert Opin Pharmacother. 2019 Nov;20(16):1943-1951. doi: 10.1080/14656566.2019.1657093. Epub 2019 Aug 26.
  • PMID: 27785927
    Winton EF, Kota V: Momelotinib in myelofibrosis: JAK1/2 inhibitor with a role in treating and understanding the anemia. Future Oncol. 2017 Feb;13(5):395-407. doi: 10.2217/fon-2016-0417. Epub 2016 Oct 27.
  • PMID: 35045875
    Chifotides HT, Bose P, Verstovsek S: Momelotinib: an emerging treatment for myelofibrosis patients with anemia. J Hematol Oncol. 2022 Jan 19;15(1):7. doi: 10.1186/s13045-021-01157-4.

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