Selinexor

DB11942

small molecule approved investigational

Deskripsi

Selinexor is a first-in-class selective inhibitor of nuclear transport (SINE) compound. Selinexor, in combination with bortezomib and dexamethasone, is currently approved for the treatment of multiple myeloma, a type of cancer formed from antibody-producing plasma cells.L7117,L7120,L10145 This condition is typically treated with high dose bortezomib and dexamethasone chemotherapy followed by an autologous stem-cell transplant. Other chemotherapies for multiple myeloma include lenalidomide and dexamethasone, thalidomide, and may include melphalan if the patient is not eligible for transplant.L7123 Selinexor was also granted accelerated approval for the treatment of adult patients with relapsed or refractory diffuse large B-cell lymphoma (DLBCL) that have gone through at least 2 lines of systemic therapy.L10145

The FDA approved Selinexor in June 2019.L10145 The use of selinexor in combination with bortezomib and dexamethasone was approved by Health Canada in June 2022 for the treatment of multiple myeloma in adult patients who have received at least one prior therapy.

Struktur Molekul 2D

Berat 443.313
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Selinexor has a mean half-life of elimination of 6-8 hours.[label,A180151,A180154,A180157]
Volume Distribusi The mean apparent volume of distribution is 125 L.[label] A phase 1 study reported mean apparent volumes of distribution ranging from 1.9-2.9 L/kg in their investigation of food and formulation effects.[A180154]
Klirens (Clearance) Selinexor has a mean apparent clearance of 17.9 L/h.[label]

Absorpsi

A single 80 mg dose of selinexor produces a mean Cmax of 680 ng/mL and a mean AUC of 5386 ng*h/mL.label This relationship is dose proportion over the range of 3-85 mg/m2 which encompasses the range of 0.06-1.8 times the approved dosage. The official FDA labeling reports the Tmax as 4 hours but phase 1 studies have found a range of 2-4 hours.label,A180151,A180154,A180157 Administering selinexor with food, either a high or low fat meal, results in an increase in the AUC of approximately 15-20% but this is not expected to be clinically significant.A180154

Metabolisme

Selinexor is known to be metabolized through CYP3A4, UDP?glucuronosyltransferases, and glutathione S-transferases although the metabolite profile has yet to be characterized in published literature.label The primary metabolites found in urine and plasma are glucuronide conjugates.A180157

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

1 Data
  • 1. Take with or without food. Co-administration with food does not affect pharmacokinetics.

Interaksi Obat

184 Data
Pitolisant The serum concentration of Selinexor can be decreased when it is combined with Pitolisant.
Metreleptin The metabolism of Selinexor can be increased when combined with Metreleptin.
Pravastatin The excretion of Pravastatin can be decreased when combined with Selinexor.
Valsartan The excretion of Valsartan can be decreased when combined with Selinexor.
Liothyronine The excretion of Liothyronine can be decreased when combined with Selinexor.
Caspofungin The excretion of Caspofungin can be decreased when combined with Selinexor.
Ouabain The excretion of Ouabain can be decreased when combined with Selinexor.
Cholic Acid The excretion of Cholic Acid can be decreased when combined with Selinexor.
Taurocholic acid The excretion of Taurocholic acid can be decreased when combined with Selinexor.
Cholecystokinin The excretion of Cholecystokinin can be decreased when combined with Selinexor.
Gadoxetic acid The excretion of Gadoxetic acid can be decreased when combined with Selinexor.
Technetium Tc-99m mebrofenin The excretion of Technetium Tc-99m mebrofenin can be decreased when combined with Selinexor.
Sincalide The excretion of Sincalide can be decreased when combined with Selinexor.
Glecaprevir The excretion of Glecaprevir can be decreased when combined with Selinexor.
Levosalbutamol The excretion of Levosalbutamol can be decreased when combined with Selinexor.
Conjugated estrogens The excretion of Conjugated estrogens can be decreased when combined with Selinexor.
Raloxifene The excretion of Raloxifene can be decreased when combined with Selinexor.
Methotrexate The excretion of Methotrexate can be decreased when combined with Selinexor.
Testosterone The excretion of Testosterone can be decreased when combined with Selinexor.
Mycophenolate mofetil The excretion of Mycophenolate mofetil can be decreased when combined with Selinexor.
Atorvastatin The excretion of Atorvastatin can be decreased when combined with Selinexor.
Fluvastatin The excretion of Fluvastatin can be decreased when combined with Selinexor.
Paclitaxel The excretion of Paclitaxel can be decreased when combined with Selinexor.
Docetaxel The excretion of Docetaxel can be decreased when combined with Selinexor.
Liotrix The excretion of Liotrix can be decreased when combined with Selinexor.
Ambrisentan The excretion of Ambrisentan can be decreased when combined with Selinexor.
Paritaprevir The excretion of Paritaprevir can be decreased when combined with Selinexor.
Tenofovir alafenamide The excretion of Tenofovir alafenamide can be decreased when combined with Selinexor.
Selexipag The excretion of Selexipag can be decreased when combined with Selinexor.
Grazoprevir The excretion of Grazoprevir can be decreased when combined with Selinexor.
Voxilaprevir The excretion of Voxilaprevir can be decreased when combined with Selinexor.
Letermovir The excretion of Letermovir can be decreased when combined with Selinexor.
Fexofenadine The excretion of Fexofenadine can be decreased when combined with Selinexor.
Bempedoic acid The excretion of Bempedoic acid can be decreased when combined with Selinexor.
Belantamab mafodotin The excretion of Belantamab mafodotin can be decreased when combined with Selinexor.
Revefenacin Selinexor may decrease the excretion rate of Revefenacin which could result in a higher serum level.
Cenobamate The serum concentration of Selinexor can be decreased when it is combined with Cenobamate.
Ritonavir The serum concentration of Selinexor can be increased when it is combined with Ritonavir.
Haloperidol The serum concentration of Haloperidol can be increased when it is combined with Selinexor.
Tucatinib The metabolism of Tucatinib can be decreased when combined with Selinexor.
Abametapir The serum concentration of Selinexor can be increased when it is combined with Abametapir.
Satralizumab The serum concentration of Selinexor can be decreased when it is combined with Satralizumab.
Sotorasib The serum concentration of Selinexor can be decreased when it is combined with Sotorasib.
Brincidofovir The serum concentration of Brincidofovir can be increased when it is combined with Selinexor.
Erythromycin The serum concentration of Selinexor can be increased when it is combined with Erythromycin.
Simeprevir The metabolism of Selinexor can be decreased when combined with Simeprevir.
Cyclosporine The metabolism of Selinexor can be decreased when combined with Cyclosporine.
Fluvoxamine The metabolism of Selinexor can be decreased when combined with Fluvoxamine.
Fluconazole The metabolism of Selinexor can be decreased when combined with Fluconazole.
Ziprasidone The metabolism of Selinexor can be decreased when combined with Ziprasidone.
Isradipine The metabolism of Selinexor can be decreased when combined with Isradipine.
Diltiazem The metabolism of Selinexor can be decreased when combined with Diltiazem.
Clozapine The metabolism of Selinexor can be decreased when combined with Clozapine.
Ciprofloxacin The metabolism of Selinexor can be decreased when combined with Ciprofloxacin.
Nicardipine The metabolism of Selinexor can be decreased when combined with Nicardipine.
Verapamil The metabolism of Selinexor can be decreased when combined with Verapamil.
Aprepitant The metabolism of Selinexor can be decreased when combined with Aprepitant.
Isoniazid The metabolism of Selinexor can be decreased when combined with Isoniazid.
Primaquine The metabolism of Selinexor can be decreased when combined with Primaquine.
Miconazole The metabolism of Selinexor can be decreased when combined with Miconazole.
Fusidic acid The metabolism of Selinexor can be decreased when combined with Fusidic acid.
Zimelidine The metabolism of Selinexor can be decreased when combined with Zimelidine.
Dronedarone The metabolism of Selinexor can be decreased when combined with Dronedarone.
Milnacipran The metabolism of Selinexor can be decreased when combined with Milnacipran.
Isavuconazonium The metabolism of Selinexor can be decreased when combined with Isavuconazonium.
Desvenlafaxine The metabolism of Selinexor can be decreased when combined with Desvenlafaxine.
Nilvadipine The metabolism of Selinexor can be decreased when combined with Nilvadipine.
Seproxetine The metabolism of Selinexor can be decreased when combined with Seproxetine.
Linagliptin The metabolism of Selinexor can be decreased when combined with Linagliptin.
Indalpine The metabolism of Selinexor can be decreased when combined with Indalpine.
Netupitant The metabolism of Selinexor can be decreased when combined with Netupitant.
Barnidipine The metabolism of Selinexor can be decreased when combined with Barnidipine.
Benidipine The metabolism of Selinexor can be decreased when combined with Benidipine.
Venetoclax The metabolism of Selinexor can be decreased when combined with Venetoclax.
Isavuconazole The metabolism of Selinexor can be decreased when combined with Isavuconazole.
Fosnetupitant The metabolism of Selinexor can be decreased when combined with Fosnetupitant.
Berotralstat The metabolism of Selinexor can be decreased when combined with Berotralstat.
Midostaurin The metabolism of Selinexor can be decreased when combined with Midostaurin.
Voriconazole The metabolism of Selinexor can be decreased when combined with Voriconazole.
Danazol The metabolism of Selinexor can be decreased when combined with Danazol.
Nelfinavir The metabolism of Selinexor can be decreased when combined with Nelfinavir.
Indinavir The metabolism of Selinexor can be decreased when combined with Indinavir.
Terfenadine The metabolism of Selinexor can be decreased when combined with Terfenadine.
Efavirenz The metabolism of Selinexor can be decreased when combined with Efavirenz.
Ergotamine The metabolism of Selinexor can be decreased when combined with Ergotamine.
Amprenavir The metabolism of Selinexor can be decreased when combined with Amprenavir.
Delavirdine The metabolism of Selinexor can be decreased when combined with Delavirdine.
Methimazole The metabolism of Selinexor can be decreased when combined with Methimazole.
Conivaptan The metabolism of Selinexor can be decreased when combined with Conivaptan.
Tipranavir The metabolism of Selinexor can be decreased when combined with Tipranavir.
Telithromycin The metabolism of Selinexor can be decreased when combined with Telithromycin.
Ketoconazole The metabolism of Selinexor can be decreased when combined with Ketoconazole.
Atazanavir The metabolism of Selinexor can be decreased when combined with Atazanavir.
Amiodarone The metabolism of Selinexor can be decreased when combined with Amiodarone.
Nefazodone The metabolism of Selinexor can be decreased when combined with Nefazodone.
Itraconazole The metabolism of Selinexor can be decreased when combined with Itraconazole.
Clarithromycin The metabolism of Selinexor can be decreased when combined with Clarithromycin.
Saquinavir The metabolism of Selinexor can be decreased when combined with Saquinavir.
Posaconazole The metabolism of Selinexor can be decreased when combined with Posaconazole.
Darunavir The metabolism of Selinexor can be decreased when combined with Darunavir.

Target Protein

Exportin-1 XPO1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 27507877
    Alexander TB, Lacayo NJ, Choi JK, Ribeiro RC, Pui CH, Rubnitz JE: Phase I Study of Selinexor, a Selective Inhibitor of Nuclear Export, in Combination With Fludarabine and Cytarabine, in Pediatric Relapsed or Refractory Acute Leukemia. J Clin Oncol. 2016 Dec;34(34):4094-4101. doi: 10.1200/JCO.2016.67.5066. Epub 2016 Oct 31.
  • PMID: 27458288
    Gounder MM, Zer A, Tap WD, Salah S, Dickson MA, Gupta AA, Keohan ML, Loong HH, D'Angelo SP, Baker S, Condy M, Nyquist-Schultz K, Tanner L, Erinjeri JP, Jasmine FH, Friedlander S, Carlson R, Unger TJ, Saint-Martin JR, Rashal T, Ellis J, Kauffman M, Shacham S, Schwartz GK, Abdul Razak AR: Phase IB Study of Selinexor, a First-in-Class Inhibitor of Nuclear Export, in Patients With Advanced Refractory Bone or Soft Tissue Sarcoma. J Clin Oncol. 2016 Sep 10;34(26):3166-74. doi: 10.1200/JCO.2016.67.6346. Epub 2016 Jul 25.
  • PMID: 26926685
    Abdul Razak AR, Mau-Soerensen M, Gabrail NY, Gerecitano JF, Shields AF, Unger TJ, Saint-Martin JR, Carlson R, Landesman Y, McCauley D, Rashal T, Lassen U, Kim R, Stayner LA, Mirza MR, Kauffman M, Shacham S, Mahipal A: First-in-Class, First-in-Human Phase I Study of Selinexor, a Selective Inhibitor of Nuclear Export, in Patients With Advanced Solid Tumors. J Clin Oncol. 2016 Dec;34(34):4142-4150. doi: 10.1200/JCO.2015.65.3949. Epub 2016 Oct 31.
  • PMID: 29610030
    Gandhi UH, Senapedis W, Baloglu E, Unger TJ, Chari A, Vogl D, Cornell RF: Clinical Implications of Targeting XPO1-mediated Nuclear Export in Multiple Myeloma. Clin Lymphoma Myeloma Leuk. 2018 May;18(5):335-345. doi: 10.1016/j.clml.2018.03.003. Epub 2018 Mar 14.
  • PMID: 25187272
    Xia Y, Shen S, Verma IM: NF-kappaB, an active player in human cancers. Cancer Immunol Res. 2014 Sep;2(9):823-30. doi: 10.1158/2326-6066.CIR-14-0112.

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