Peringatan Keamanan

There is no information on the LD50 or overdose of berotralstat.

Berotralstat

DB15982

small molecule approved

Deskripsi

Berotralstat is a selective inhibitor of plasma kallikrein used in the prophylaxis of attacks of hereditary angioedema (HAE).L26661 It works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE.A225166 Berotralstat is strictly used to prevent, but not treat, these attacks.L26656

Developed by BioCryst Pharmaceuticals, berotralstat is marketed under the name Orladeyo as oral capsules.A225106 Berotralstat was first approved by the FDA on December 3, 2020, as the first once-daily oral therapy to prevent angioedema attacks of HAE in adults and pediatric patients 12 years and older.L26661 Berotralstat was approved by the European Commission on April 30, 2021 L41965 and by Health Canada on June 06, 2022.L41960

Struktur Molekul 2D

Berat 562.573
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following a single oral dose administration of 300 mg radiolabeled berotralstat, the median elimination half-life of berotralstat was approximately 93 hours, ranging from 39 to 152 hours.[L26661]
Volume Distribusi The blood to plasma ratio was approximately 0.92 following a single 300 mg dose administration of radiolabeled berotralstat.[L26661]
Klirens (Clearance) There is no information on the clearance rate.

Absorpsi

The steady-state of berotralstat is reached within 6 to 12 days following initial administration. After once-daily administration, the Cmax and AUC of berotralstat at steady-state is approximately five times that of the drug after a single dose. Following oral administration of berotralstat once-daily, the steady-state Cmax was 158 ng/mL (range: 110 to 234 ng/mL) at the dose of 150 mg and 97.8 ng/mL (range: 63 to 235 ng/mL) at the dose of 110 mg. The area under the curve over the dosing interval (AUCtau) was 2770 ng*hr/mL (range: 1880 to 3790 ng*hr/mL) and 1600 ng*hr/mL (range: 950 to 4170 ng*hr/mL) at the dose of 110 mg. The median Tmax is 2 hours in a fasted state and a high-fat meal delays the Tmax to 5 hours. The Tmax can range from 1 to 8 hours.L26661

Metabolisme

Berotralstat is metabolized by CYP2D6 and CYP3A4. The metabolic pathway and the metabolites of berotralstat have not yet been characterized. Following a single oral dose administration of 300 mg radiolabeled berotralstat, about 34% of the total plasma radioactivity accounted for the unchanged drug while about eight detectable metabolites accounted for 1.8 to 7.8% of the total radioactivity.L26661

Rute Eliminasi

Following a single oral dose administration of 300 mg radiolabeled berotralstat, approximately 9% of the drug was excreted in the urine, where 1.8 to 4.7% of the total radiolabeled compound accounted for the unchanged parent drug. About 79% of the drug was excreted in feces.L26661

Interaksi Makanan

1 Data
  • 1. Take with food. This is instructed by the prescribing information of berotralstat. A high-fat meal had no significant effects on the Cmax and AUC of berotralstat, but the Tmax was delayed by 3 hours.

Interaksi Obat

1103 Data
Ranolazine The serum concentration of Berotralstat can be increased when it is combined with Ranolazine.
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Berotralstat.
Everolimus The metabolism of Everolimus can be decreased when combined with Berotralstat.
Flibanserin The metabolism of Flibanserin can be decreased when combined with Berotralstat.
Ivabradine The metabolism of Ivabradine can be decreased when combined with Berotralstat.
Ivacaftor The metabolism of Ivacaftor can be decreased when combined with Berotralstat.
Lurasidone The metabolism of Lurasidone can be decreased when combined with Berotralstat.
Naloxegol The metabolism of Naloxegol can be decreased when combined with Berotralstat.
Olaparib The metabolism of Olaparib can be decreased when combined with Berotralstat.
Sonidegib The metabolism of Sonidegib can be decreased when combined with Berotralstat.
Avanafil The metabolism of Avanafil can be decreased when combined with Berotralstat.
Eplerenone The metabolism of Eplerenone can be decreased when combined with Berotralstat.
Ziprasidone The risk or severity of QTc prolongation can be increased when Berotralstat is combined with Ziprasidone.
Anagrelide The risk or severity of QTc prolongation can be increased when Berotralstat is combined with Anagrelide.
Disopyramide The risk or severity of QTc prolongation can be increased when Berotralstat is combined with Disopyramide.
Clemastine The risk or severity of QTc prolongation can be increased when Berotralstat is combined with Clemastine.
Ibutilide The risk or severity of QTc prolongation can be increased when Berotralstat is combined with Ibutilide.
Valproic acid The risk or severity of QTc prolongation can be increased when Berotralstat is combined with Valproic acid.
Grepafloxacin The risk or severity of QTc prolongation can be increased when Berotralstat is combined with Grepafloxacin.
Cisapride The risk or severity of QTc prolongation can be increased when Berotralstat is combined with Cisapride.
Trovafloxacin The risk or severity of QTc prolongation can be increased when Berotralstat is combined with Trovafloxacin.
Cocaine The risk or severity of QTc prolongation can be increased when Berotralstat is combined with Cocaine.
Sparfloxacin The risk or severity of QTc prolongation can be increased when Berotralstat is combined with Sparfloxacin.
Halofantrine The risk or severity of QTc prolongation can be increased when Berotralstat is combined with Halofantrine.
Lithium cation The risk or severity of QTc prolongation can be increased when Berotralstat is combined with Lithium cation.
Temafloxacin The risk or severity of QTc prolongation can be increased when Berotralstat is combined with Temafloxacin.
Asenapine The risk or severity of QTc prolongation can be increased when Berotralstat is combined with Asenapine.
Artemether The risk or severity of QTc prolongation can be increased when Berotralstat is combined with Artemether.
Lumefantrine The risk or severity of QTc prolongation can be increased when Berotralstat is combined with Lumefantrine.
Macimorelin The risk or severity of QTc prolongation can be increased when Berotralstat is combined with Macimorelin.
Terodiline The risk or severity of QTc prolongation can be increased when Berotralstat is combined with Terodiline.
Leuprolide The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Berotralstat.
Goserelin The risk or severity of QTc prolongation can be increased when Goserelin is combined with Berotralstat.
Azithromycin The risk or severity of QTc prolongation can be increased when Azithromycin is combined with Berotralstat.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Moxifloxacin is combined with Berotralstat.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Sulfisoxazole is combined with Berotralstat.
Sulpiride The risk or severity of QTc prolongation can be increased when Sulpiride is combined with Berotralstat.
Nimodipine The risk or severity of QTc prolongation can be increased when Nimodipine is combined with Berotralstat.
Droperidol The risk or severity of QTc prolongation can be increased when Droperidol is combined with Berotralstat.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Berotralstat.
Ciprofloxacin The risk or severity of QTc prolongation can be increased when Ciprofloxacin is combined with Berotralstat.
Fluorouracil The risk or severity of QTc prolongation can be increased when Fluorouracil is combined with Berotralstat.
Perflutren The risk or severity of QTc prolongation can be increased when Perflutren is combined with Berotralstat.
Atropine The risk or severity of QTc prolongation can be increased when Atropine is combined with Berotralstat.
Efavirenz The risk or severity of QTc prolongation can be increased when Efavirenz is combined with Berotralstat.
Adenosine The risk or severity of QTc prolongation can be increased when Adenosine is combined with Berotralstat.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Berotralstat.
Carbinoxamine The risk or severity of QTc prolongation can be increased when Carbinoxamine is combined with Berotralstat.
Roxithromycin The risk or severity of QTc prolongation can be increased when Roxithromycin is combined with Berotralstat.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Nalidixic acid is combined with Berotralstat.
Cinoxacin The risk or severity of QTc prolongation can be increased when Cinoxacin is combined with Berotralstat.
Granisetron The risk or severity of QTc prolongation can be increased when Granisetron is combined with Berotralstat.
Levosimendan The risk or severity of QTc prolongation can be increased when Levosimendan is combined with Berotralstat.
Desloratadine The risk or severity of QTc prolongation can be increased when Desloratadine is combined with Berotralstat.
Telithromycin The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Berotralstat.
Lomefloxacin The risk or severity of QTc prolongation can be increased when Lomefloxacin is combined with Berotralstat.
Dimenhydrinate The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Berotralstat.
Emedastine The risk or severity of QTc prolongation can be increased when Emedastine is combined with Berotralstat.
Primaquine The risk or severity of QTc prolongation can be increased when Primaquine is combined with Berotralstat.
Papaverine The risk or severity of QTc prolongation can be increased when Papaverine is combined with Berotralstat.
Levofloxacin The risk or severity of QTc prolongation can be increased when Levofloxacin is combined with Berotralstat.
Gemifloxacin The risk or severity of QTc prolongation can be increased when Gemifloxacin is combined with Berotralstat.
Ofloxacin The risk or severity of QTc prolongation can be increased when Ofloxacin is combined with Berotralstat.
Probucol The risk or severity of QTc prolongation can be increased when Probucol is combined with Berotralstat.
Aceprometazine The risk or severity of QTc prolongation can be increased when Aceprometazine is combined with Berotralstat.
Terlipressin The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Berotralstat.
Prenylamine The risk or severity of QTc prolongation can be increased when Prenylamine is combined with Berotralstat.
Fluspirilene The risk or severity of QTc prolongation can be increased when Fluspirilene is combined with Berotralstat.
Azimilide The risk or severity of QTc prolongation can be increased when Azimilide is combined with Berotralstat.
Pracinostat The risk or severity of QTc prolongation can be increased when Pracinostat is combined with Berotralstat.
Technetium Tc-99m ciprofloxacin The risk or severity of QTc prolongation can be increased when Technetium Tc-99m ciprofloxacin is combined with Berotralstat.
Garenoxacin The risk or severity of QTc prolongation can be increased when Garenoxacin is combined with Berotralstat.
Tedisamil The risk or severity of QTc prolongation can be increased when Tedisamil is combined with Berotralstat.
Tucidinostat The risk or severity of QTc prolongation can be increased when Tucidinostat is combined with Berotralstat.
Telavancin The risk or severity of QTc prolongation can be increased when Telavancin is combined with Berotralstat.
Nemonoxacin The risk or severity of QTc prolongation can be increased when Nemonoxacin is combined with Berotralstat.
Nilvadipine The risk or severity of QTc prolongation can be increased when Nilvadipine is combined with Berotralstat.
Antazoline The risk or severity of QTc prolongation can be increased when Antazoline is combined with Berotralstat.
Bedaquiline The risk or severity of QTc prolongation can be increased when Bedaquiline is combined with Berotralstat.
Fendiline The risk or severity of QTc prolongation can be increased when Fendiline is combined with Berotralstat.
Eperisone The risk or severity of QTc prolongation can be increased when Eperisone is combined with Berotralstat.
Butriptyline The risk or severity of QTc prolongation can be increased when Butriptyline is combined with Berotralstat.
Melperone The risk or severity of QTc prolongation can be increased when Melperone is combined with Berotralstat.
Benidipine The risk or severity of QTc prolongation can be increased when Benidipine is combined with Berotralstat.
Delamanid The risk or severity of QTc prolongation can be increased when Delamanid is combined with Berotralstat.
Amifampridine The risk or severity of QTc prolongation can be increased when Amifampridine is combined with Berotralstat.
Mocetinostat The risk or severity of QTc prolongation can be increased when Mocetinostat is combined with Berotralstat.
Entinostat The risk or severity of QTc prolongation can be increased when Entinostat is combined with Berotralstat.
CUDC-101 The risk or severity of QTc prolongation can be increased when CUDC-101 is combined with Berotralstat.
Simendan The risk or severity of QTc prolongation can be increased when Simendan is combined with Berotralstat.
Ricolinostat The risk or severity of QTc prolongation can be increased when Ricolinostat is combined with Berotralstat.
Mizolastine The risk or severity of QTc prolongation can be increased when Mizolastine is combined with Berotralstat.
Abexinostat The risk or severity of QTc prolongation can be increased when Abexinostat is combined with Berotralstat.
Oxatomide The risk or severity of QTc prolongation can be increased when Oxatomide is combined with Berotralstat.
Sitafloxacin The risk or severity of QTc prolongation can be increased when Sitafloxacin is combined with Berotralstat.
Sultopride The risk or severity of QTc prolongation can be increased when Sultopride is combined with Berotralstat.
Otilonium The risk or severity of QTc prolongation can be increased when Otilonium is combined with Berotralstat.
Nizofenone The risk or severity of QTc prolongation can be increased when Nizofenone is combined with Berotralstat.
Bunaftine The risk or severity of QTc prolongation can be increased when Bunaftine is combined with Berotralstat.
Lorcainide The risk or severity of QTc prolongation can be increased when Lorcainide is combined with Berotralstat.

Target Protein

Plasma kallikrein KLKB1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 31635497
    Hwang JR, Hwang G, Johri A, Craig T: Oral plasma kallikrein inhibitor BCX7353 for treatment of hereditary angioedema. Immunotherapy. 2019 Dec;11(17):1439-1444. doi: 10.2217/imt-2019-0128. Epub 2019 Oct 22.
  • PMID: 30044938
    Aygoren-Pursun E, Bygum A, Grivcheva-Panovska V, Magerl M, Graff J, Steiner UC, Fain O, Huissoon A, Kinaciyan T, Farkas H, Lleonart R, Longhurst HJ, Rae W, Triggiani M, Aberer W, Cancian M, Zanichelli A, Smith WB, Baeza ML, Du-Thanh A, Gompels M, Gonzalez-Quevedo T, Greve J, Guilarte M, Katelaris C, Dobo S, Cornpropst M, Clemons D, Fang L, Collis P, Sheridan W, Maurer M, Cicardi M: Oral Plasma Kallikrein Inhibitor for Prophylaxis in Hereditary Angioedema. N Engl J Med. 2018 Jul 26;379(4):352-362. doi: 10.1056/NEJMoa1716995.
  • PMID: 29423395
    Schmaier AH: Plasma Prekallikrein: Its Role in Hereditary Angioedema and Health and Disease. Front Med (Lausanne). 2018 Jan 25;5:3. doi: 10.3389/fmed.2018.00003. eCollection 2018.

Contoh Produk & Brand

Produk: 5 • International brands: 1
Produk
  • Orladeyo
    Capsule • 150 mg/1 • Oral • US • Approved
  • Orladeyo
    Capsule • 110 mg/1 • Oral • US • Approved
  • Orladeyo
    Capsule • 150 mg • Oral • EU • Approved
  • Orladeyo
    Capsule • 150 mg • Oral • EU • Approved
  • Orladeyo
    Capsule • 150 mg • Oral • Canada • Approved
International Brands
  • Orladeyo — BioCryst

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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