Peringatan Keamanan

Contra-indicated in pregnancy, and moderate to severe hepatic insufficiency (Child-Pugh category B or C). Severe GI adverse reactions may occur.

Lomitapide

DB08827

small molecule approved investigational

Deskripsi

Lomitapide is a microsomal triglyceride transfer protein (MTP) inhibitor used in homozygous familial hypercholesterolemia (HoFH) patients. It is marketed under the name Juxtapid (R).

Struktur Molekul 2D

Berat 693.7204
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Lomitapide half-life is about 39.7 hours.
Volume Distribusi The steady state volume of distribution is about 985-1292 L.
Klirens (Clearance) -

Absorpsi

In healthy patients, time to maximum lomitapide concentration is about 6 hours with a single dose of 60 mg. Lomitapide has an approximate absolute bioavailability of 7%.

Metabolisme

Lomitapide is mainly metabolized by CYP3A4 to it's inactive metabolites, M1 and M3. CYP enzymes that metabolize lomitapide to a minor extent include CYP 1A2,2B6,2C8,2C19.

Rute Eliminasi

About 52.9-59.5% is eliminated by the urine and 33.4-35.1% is eliminated by the feces.

Interaksi Makanan

2 Data
  • 1. Avoid grapefruit products.
  • 2. Take with food. Food decreases the risk of GI side effects.

Interaksi Obat

612 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Lomitapide.
Modafinil The metabolism of Lomitapide can be increased when combined with Modafinil.
Armodafinil The metabolism of Lomitapide can be increased when combined with Armodafinil.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Lomitapide.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Lomitapide.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Lomitapide.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Lomitapide.
Cimetidine The metabolism of Lomitapide can be decreased when combined with Cimetidine.
Somatostatin The metabolism of Lomitapide can be decreased when combined with Somatostatin.
Glecaprevir The metabolism of Lomitapide can be decreased when combined with Glecaprevir.
Sarilumab The metabolism of Lomitapide can be decreased when combined with Sarilumab.
Methimazole The metabolism of Lomitapide can be decreased when combined with Methimazole.
Propofol The metabolism of Lomitapide can be decreased when combined with Propofol.
Quinupristin The metabolism of Lomitapide can be decreased when combined with Quinupristin.
Dalfopristin The metabolism of Lomitapide can be decreased when combined with Dalfopristin.
Vapreotide The metabolism of Lomitapide can be decreased when combined with Vapreotide.
Dovitinib The metabolism of Lomitapide can be decreased when combined with Dovitinib.
Pasireotide The metabolism of Lomitapide can be decreased when combined with Pasireotide.
Lanreotide The metabolism of Lomitapide can be decreased when combined with Lanreotide.
Acalabrutinib The metabolism of Lomitapide can be decreased when combined with Acalabrutinib.
Citalopram The metabolism of Lomitapide can be decreased when combined with Citalopram.
Acetaminophen The metabolism of Lomitapide can be decreased when combined with Acetaminophen.
Mirtazapine The metabolism of Lomitapide can be decreased when combined with Mirtazapine.
Roxithromycin The metabolism of Lomitapide can be decreased when combined with Roxithromycin.
Quinidine The metabolism of Lomitapide can be decreased when combined with Quinidine.
Buprenorphine The metabolism of Lomitapide can be decreased when combined with Buprenorphine.
Glyburide The metabolism of Lomitapide can be decreased when combined with Glyburide.
Bicalutamide The metabolism of Lomitapide can be decreased when combined with Bicalutamide.
Orphenadrine The metabolism of Lomitapide can be decreased when combined with Orphenadrine.
Dexamethasone The metabolism of Lomitapide can be decreased when combined with Dexamethasone.
Dasatinib The metabolism of Lomitapide can be decreased when combined with Dasatinib.
Lapatinib The metabolism of Lomitapide can be decreased when combined with Lapatinib.
Cyproterone acetate The metabolism of Lomitapide can be decreased when combined with Cyproterone acetate.
Dapoxetine The metabolism of Lomitapide can be decreased when combined with Dapoxetine.
Clevidipine The metabolism of Lomitapide can be decreased when combined with Clevidipine.
Fosaprepitant The metabolism of Lomitapide can be decreased when combined with Fosaprepitant.
Ivacaftor The metabolism of Lomitapide can be decreased when combined with Ivacaftor.
Rilpivirine The metabolism of Lomitapide can be decreased when combined with Rilpivirine.
Ceritinib The metabolism of Lomitapide can be decreased when combined with Ceritinib.
Palbociclib The metabolism of Lomitapide can be decreased when combined with Palbociclib.
Olaparib The metabolism of Lomitapide can be decreased when combined with Olaparib.
Manidipine The metabolism of Lomitapide can be decreased when combined with Manidipine.
Alpelisib The metabolism of Lomitapide can be decreased when combined with Alpelisib.
Rucaparib The metabolism of Lomitapide can be decreased when combined with Rucaparib.
Piperaquine The metabolism of Lomitapide can be decreased when combined with Piperaquine.
Siltuximab The metabolism of Lomitapide can be decreased when combined with Siltuximab.
Ranolazine The metabolism of Lomitapide can be decreased when combined with Ranolazine.
Osilodrostat The metabolism of Lomitapide can be decreased when combined with Osilodrostat.
Ticagrelor The metabolism of Lomitapide can be decreased when combined with Ticagrelor.
Bifonazole The metabolism of Lomitapide can be decreased when combined with Bifonazole.
Remdesivir The metabolism of Lomitapide can be decreased when combined with Remdesivir.
Fluoxetine The metabolism of Lomitapide can be decreased when combined with Fluoxetine.
Ginkgo biloba The metabolism of Lomitapide can be decreased when combined with Ginkgo biloba.
Ethambutol The metabolism of Lomitapide can be decreased when combined with Ethambutol.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Lomitapide.
Pazopanib The metabolism of Lomitapide can be decreased when combined with Pazopanib.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Lomitapide.
Silodosin The excretion of Silodosin can be decreased when combined with Lomitapide.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Lomitapide.
Phenytoin The metabolism of Lomitapide can be increased when combined with Phenytoin.
Fosphenytoin The metabolism of Lomitapide can be increased when combined with Fosphenytoin.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Lomitapide.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Lomitapide.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Lomitapide.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Lomitapide.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Lomitapide.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Lomitapide.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Lomitapide.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Lomitapide.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Lomitapide.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Lomitapide.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Lomitapide.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Lomitapide.
Metreleptin The metabolism of Lomitapide can be increased when combined with Metreleptin.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Lomitapide.
Colestipol Colestipol can cause a decrease in the absorption of Lomitapide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sevelamer Sevelamer can cause a decrease in the absorption of Lomitapide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colesevelam Colesevelam can cause a decrease in the absorption of Lomitapide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cholestyramine Cholestyramine can cause a decrease in the absorption of Lomitapide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Lomitapide.
Simvastatin The serum concentration of Simvastatin can be increased when it is combined with Lomitapide.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Lomitapide.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Lomitapide.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Lomitapide.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Lomitapide.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Lomitapide.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Lomitapide.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Lomitapide.
Tacrolimus The metabolism of Lomitapide can be decreased when combined with Tacrolimus.
Crizotinib The metabolism of Lomitapide can be decreased when combined with Crizotinib.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Lomitapide.
Mipomersen Lomitapide may increase the hepatotoxic activities of Mipomersen.
Vincristine The excretion of Vincristine can be decreased when combined with Lomitapide.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Lomitapide.
Ethanol Ethanol may increase the hepatotoxic activities of Lomitapide.
Betrixaban The serum concentration of Betrixaban can be increased when it is combined with Lomitapide.
Pitolisant The serum concentration of Lomitapide can be decreased when it is combined with Pitolisant.
Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Lomitapide.
Tenofovir disoproxil The serum concentration of Tenofovir disoproxil can be increased when it is combined with Lomitapide.
Mannitol The serum concentration of Mannitol can be increased when it is combined with Lomitapide.

Target Protein

Microsomal triglyceride transfer protein large subunit MTTP

Referensi & Sumber

Artikel (PubMed)
  • PMID: 23122768
    Cuchel M, Meagher EA, du Toit Theron H, Blom DJ, Marais AD, Hegele RA, Averna MR, Sirtori CR, Shah PK, Gaudet D, Stefanutti C, Vigna GB, Du Plessis AM, Propert KJ, Sasiela WJ, Bloedon LT, Rader DJ: Efficacy and safety of a microsomal triglyceride transfer protein inhibitor in patients with homozygous familial hypercholesterolaemia: a single-arm, open-label, phase 3 study. Lancet. 2013 Jan 5;381(9860):40-6. doi: 10.1016/S0140-6736(12)61731-0. Epub 2012 Nov 2.
  • PMID: 17215532
    Cuchel M, Bloedon LT, Szapary PO, Kolansky DM, Wolfe ML, Sarkis A, Millar JS, Ikewaki K, Siegelman ES, Gregg RE, Rader DJ: Inhibition of microsomal triglyceride transfer protein in familial hypercholesterolemia. N Engl J Med. 2007 Jan 11;356(2):148-56.

Contoh Produk & Brand

Produk: 19 • International brands: 1
Produk
  • Juxtapid
    Capsule • 5 mg/1 • Oral • US • Approved
  • Juxtapid
    Capsule • 10 mg/1 • Oral • US • Approved
  • Juxtapid
    Capsule • 5 mg • Oral • Canada • Approved
  • Juxtapid
    Capsule • 10 mg • Oral • Canada • Approved
  • Juxtapid
    Capsule • 20 mg • Oral • Canada • Approved
  • Juxtapid
    Capsule • 20 mg/1 • Oral • US • Approved
  • Juxtapid
    Capsule • 30 mg/1 • Oral • US • Approved
  • Juxtapid
    Capsule • 5 mg/1 • Oral • US • Approved
Menampilkan 8 dari 19 produk.
International Brands
  • Lojuxta

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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