Peringatan Keamanan

Patients experiencing an overdose may present with hyperglycemia, nausea, asthenia, and rash. There is no antidote for an overdose of alpelisib so patients should be treated symptomatically.L6652

Data regarding an LD50 is not readily available.L41389 In clinical trials, patients were given doses of up to 450mg once daily.L6652

Alpelisib

DB12015

small molecule approved investigational

Deskripsi

Alpelisib is a phosphatidylinositol 3-kinase (PI3K) inhibitor with potent antitumor activity. It works by selectively inhibiting class I PI3K p110? A179203, which is the catalytic subunit of PI3K, a lipid kinase that plays a role in various biological processes, including proliferation, survival, differentiation, and metabolism. Alpelisib was designed to target this enzyme that appears to be mutated at a rate of nearly 30% in human cancers, leading to hyperactivation.A179209

There are several isoform-specific PI3K inhibitors that are under clinical development or currently approved, such as idelalisib used for chronic lymphocytic leukemia (CLL).A179209 Approved by the FDA in May 2019, alpelisib is the first approved PI3K inhibitor indicated for the treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CA-mutated, advanced or metastatic breast cancer in combination with fulvestrant for postmenopausal women and male patients. To initiate alpelisib therapy, it is required that the presence of a PIK3CA mutation in the tissue and/or liquid biopsy sample collection should be confirmed via FDA-approved diagnostic tests. Alpelisib is marketed under the trade name Piqray and is available as oral tablets. Studies evaluating the therapeutic effectiveness of alpelisib in other cancers, such as ovarian cancer A179200 and colorectal cancer A179203, are under ongoing investigations.

Alpelisib was granted FDA approval on 24 May 2019.L6652 In April 2022, the FDA granted the use of alpelisib in the treatment of PIK3CA-Related Overgrowth Spectrum (PROS) in adults and children who require systemic therapy.L41384

Struktur Molekul 2D

Berat 441.47
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 half life of alprelisib is 8 to 9 hours.[L6652]
Volume Distribusi The apparent volume of distribution at steady state is 114L.[L6652]
Klirens (Clearance) The mean apparent oral clearance was 39.0L/h.[A179254] The predicted clearance is 9.2L/hr under fed conditions.[L6652]

Absorpsi

Alpelisib reached a peak concentration in plasma of 1320±912ng/mL after 2 hours.A179254 Alpelisib has an AUClast of 11,100±3760h ng/mL and an AUCINF of 11,100±3770h ng/mL.A179254 A large, high fat meal increases the AUC by 73% and Cmax by 84% while a small, low fat meal increases the AUC by 77% and Cmax by 145%.L6652

Metabolisme

Alpelisib is metabolized by hydrolysis reactions to form the primary metabolite. It is also metabolized by CYP3A4.L6652 The full metabolism of Alpelisib has yet to be determined but a series of reactions have been proposed.A179254,A179257 The main metabolic reaction is the substitution of an amine group on alpelisib for a hydroxyl group to form a metabolite known as M4A179254,A179257 or BZG791.L6652 Alpelisib can also be glucuronidated to form the M1 and M12 metabolites.A179254,A179257

Rute Eliminasi

36% of an oral dose is eliminated as unchanged drug in the feces and 32% as the primary metabolite BZG791 in the feces. About 2% of an oral dose is eliminated in the urine as unchanged drug and 7.1% as the primary metabolite BZG791. In total 81% of an oral dose is eliminated in the feces and 14% is eliminated in the urine.L6652

Interaksi Makanan

3 Data
  • 1. Exercise caution with St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of alpelisib.
  • 2. Take at the same time every day.
  • 3. Take with food. Food does not significantly affect the AUC of alpelisib.

Interaksi Obat

857 Data
Modafinil The metabolism of Alpelisib can be increased when combined with Modafinil.
Armodafinil The metabolism of Alpelisib can be increased when combined with Armodafinil.
Lomitapide The metabolism of Lomitapide can be decreased when combined with Alpelisib.
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Alpelisib.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Alpelisib.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Alpelisib.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Alpelisib.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Alpelisib.
Colchicine The metabolism of Colchicine can be decreased when combined with Alpelisib.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Alpelisib.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Alpelisib.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Alpelisib.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Alpelisib.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Alpelisib.
Metreleptin The metabolism of Alpelisib can be increased when combined with Metreleptin.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Alpelisib.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Alpelisib.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Alpelisib.
Perampanel The metabolism of Perampanel can be increased when combined with Alpelisib.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Alpelisib.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Alpelisib.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Alpelisib.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Alpelisib.
Crizotinib The metabolism of Alpelisib can be decreased when combined with Crizotinib.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Alpelisib.
Erlotinib The serum concentration of Erlotinib can be decreased when it is combined with Alpelisib.
Pitolisant The serum concentration of Alpelisib can be decreased when it is combined with Pitolisant.
Segesterone acetate The metabolism of Segesterone acetate can be increased when combined with Alpelisib.
Cholesterol Cholesterol may increase the excretion rate of Alpelisib which could result in a lower serum level and potentially a reduction in efficacy.
Etonogestrel The metabolism of Etonogestrel can be increased when combined with Alpelisib.
Levonorgestrel The metabolism of Levonorgestrel can be increased when combined with Alpelisib.
Ethynodiol diacetate The metabolism of Ethynodiol diacetate can be increased when combined with Alpelisib.
Octylphenoxy polyethoxyethanol The metabolism of Octylphenoxy polyethoxyethanol can be increased when combined with Alpelisib.
Trestolone The metabolism of Trestolone can be increased when combined with Alpelisib.
Norelgestromin The metabolism of Norelgestromin can be increased when combined with Alpelisib.
Gestodene The metabolism of Gestodene can be increased when combined with Alpelisib.
Hydroxyprogesterone caproate The metabolism of Hydroxyprogesterone caproate can be increased when combined with Alpelisib.
Dienogest The metabolism of Dienogest can be increased when combined with Alpelisib.
Norethynodrel The metabolism of Norethynodrel can be increased when combined with Alpelisib.
Norgestrel The metabolism of Norgestrel can be increased when combined with Alpelisib.
Cloprostenol The metabolism of Cloprostenol can be increased when combined with Alpelisib.
Gestrinone The metabolism of Gestrinone can be increased when combined with Alpelisib.
Nomegestrol The metabolism of Nomegestrol can be increased when combined with Alpelisib.
Gossypol The metabolism of Gossypol can be increased when combined with Alpelisib.
Ormeloxifene The metabolism of Ormeloxifene can be increased when combined with Alpelisib.
Chlormadinone The metabolism of Chlormadinone can be increased when combined with Alpelisib.
Norgestrienone The metabolism of Norgestrienone can be increased when combined with Alpelisib.
Quingestanol The metabolism of Quingestanol can be increased when combined with Alpelisib.
Demegestone The metabolism of Demegestone can be increased when combined with Alpelisib.
Etynodiol The metabolism of Etynodiol can be increased when combined with Alpelisib.
Nomegestrol acetate The metabolism of Nomegestrol acetate can be increased when combined with Alpelisib.
Norethindrone enanthate The metabolism of Norethindrone enanthate can be increased when combined with Alpelisib.
Ulipristal The metabolism of Ulipristal can be increased when combined with Alpelisib.
Megestrol acetate The metabolism of Megestrol acetate can be increased when combined with Alpelisib.
Nafcillin The metabolism of Alpelisib can be increased when combined with Nafcillin.
Avasimibe The metabolism of Alpelisib can be increased when combined with Avasimibe.
Echinacea The metabolism of Alpelisib can be increased when combined with Echinacea.
Dofetilide The metabolism of Dofetilide can be increased when combined with Alpelisib.
Theophylline The metabolism of Theophylline can be increased when combined with Alpelisib.
Busulfan The metabolism of Busulfan can be increased when combined with Alpelisib.
Pimozide The metabolism of Pimozide can be increased when combined with Alpelisib.
Aminophylline The metabolism of Aminophylline can be increased when combined with Alpelisib.
Tianeptine The metabolism of Tianeptine can be increased when combined with Alpelisib.
Rifabutin The metabolism of Alpelisib can be increased when combined with Rifabutin.
Felbamate The metabolism of Alpelisib can be increased when combined with Felbamate.
Oritavancin The metabolism of Alpelisib can be increased when combined with Oritavancin.
Rufinamide The metabolism of Alpelisib can be increased when combined with Rufinamide.
Glycerol phenylbutyrate The metabolism of Alpelisib can be increased when combined with Glycerol phenylbutyrate.
Eslicarbazepine acetate The metabolism of Alpelisib can be increased when combined with Eslicarbazepine acetate.
Sarilumab The metabolism of Alpelisib can be increased when combined with Sarilumab.
Acalabrutinib The metabolism of Acalabrutinib can be increased when combined with Alpelisib.
Topiramate The metabolism of Alpelisib can be increased when combined with Topiramate.
Cobimetinib The metabolism of Cobimetinib can be increased when combined with Alpelisib.
Sirolimus The metabolism of Sirolimus can be increased when combined with Alpelisib.
Digitoxin The metabolism of Digitoxin can be increased when combined with Alpelisib.
Everolimus The metabolism of Everolimus can be increased when combined with Alpelisib.
Temsirolimus The metabolism of Temsirolimus can be increased when combined with Alpelisib.
Vinblastine The metabolism of Vinblastine can be increased when combined with Alpelisib.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Alpelisib.
Docetaxel The metabolism of Docetaxel can be increased when combined with Alpelisib.
Irinotecan The metabolism of Irinotecan can be increased when combined with Alpelisib.
Romidepsin The metabolism of Romidepsin can be increased when combined with Alpelisib.
Axitinib The metabolism of Axitinib can be increased when combined with Alpelisib.
Clomipramine The metabolism of Clomipramine can be increased when combined with Alpelisib.
Methotrexate The metabolism of Methotrexate can be increased when combined with Alpelisib.
Vinorelbine The metabolism of Vinorelbine can be increased when combined with Alpelisib.
Vincristine The metabolism of Vincristine can be increased when combined with Alpelisib.
Thiotepa The metabolism of Thiotepa can be increased when combined with Alpelisib.
Vinflunine The metabolism of Vinflunine can be increased when combined with Alpelisib.
Zanubrutinib The metabolism of Zanubrutinib can be increased when combined with Alpelisib.
Vindesine The metabolism of Vindesine can be increased when combined with Alpelisib.
Panobinostat The metabolism of Panobinostat can be increased when combined with Alpelisib.
Sonidegib The metabolism of Sonidegib can be increased when combined with Alpelisib.
Neratinib The metabolism of Neratinib can be increased when combined with Alpelisib.
Copanlisib The metabolism of Copanlisib can be increased when combined with Alpelisib.
Pexidartinib The metabolism of Pexidartinib can be increased when combined with Alpelisib.
Idelalisib The metabolism of Idelalisib can be increased when combined with Alpelisib.
Ixabepilone The metabolism of Ixabepilone can be increased when combined with Alpelisib.
Ixazomib The metabolism of Ixazomib can be increased when combined with Alpelisib.
Clonidine The metabolism of Clonidine can be increased when combined with Alpelisib.

Target Protein

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform PIK3CA

Referensi & Sumber

Artikel (PubMed)
  • PMID: 30880072
    Konstantinopoulos PA, Barry WT, Birrer M, Westin SN, Cadoo KA, Shapiro GI, Mayer EL, O'Cearbhaill RE, Coleman RL, Kochupurakkal B, Whalen C, Curtis J, Farooq S, Luo W, Eismann J, Buss MK, Aghajanian C, Mills GB, Palakurthi S, Kirschmeier P, Liu J, Cantley LC, Kaufmann SH, Swisher EM, D'Andrea AD, Winer E, Wulf GM, Matulonis UA: Olaparib and alpha-specific PI3K inhibitor alpelisib for patients with epithelial ovarian cancer: a dose-escalation and dose-expansion phase 1b trial. Lancet Oncol. 2019 Apr;20(4):570-580. doi: 10.1016/S1470-2045(18)30905-7. Epub 2019 Mar 14.
  • PMID: 30167089
    Rodon J, Curigliano G, Delord JP, Harb W, Azaro A, Han Y, Wilke C, Donnet V, Sellami D, Beck T: A Phase Ib, open-label, dose-finding study of alpelisib in combination with paclitaxel in patients with advanced solid tumors. Oncotarget. 2018 Aug 3;9(60):31709-31718. doi: 10.18632/oncotarget.25854. eCollection 2018 Aug 3.
  • PMID: 29109464
    Yang X, Zhang X, Huang M, Song K, Li X, Huang M, Meng L, Zhang J: New Insights into PI3K Inhibitor Design using X-ray Structures of PI3Kalpha Complexed with a Potent Lead Compound. Sci Rep. 2017 Nov 6;7(1):14572. doi: 10.1038/s41598-017-15260-5.
  • PMID: 26254025
    James A, Blumenstein L, Glaenzel U, Jin Y, Demailly A, Jakab A, Hansen R, Hazell K, Mehta A, Trandafir L, Swart P: Absorption, distribution, metabolism, and excretion of (14)CBYL719 (alpelisib) in healthy male volunteers. Cancer Chemother Pharmacol. 2015 Oct;76(4):751-60. doi: 10.1007/s00280-015-2842-4. Epub 2015 Aug 8.
  • PMID: 28566285
    James AD, Marvalin C, Luneau A, Meissner A, Camenisch G: Comparison of (19)F NMR and (14)C Measurements for the Assessment of ADME of BYL719 (Alpelisib) in Humans. Drug Metab Dispos. 2017 Aug;45(8):900-907. doi: 10.1124/dmd.117.075424. Epub 2017 May 31.
  • PMID: 24617631
    De Buck SS, Jakab A, Boehm M, Bootle D, Juric D, Quadt C, Goggin TK: Population pharmacokinetics and pharmacodynamics of BYL719, a phosphoinositide 3-kinase antagonist, in adult patients with advanced solid malignancies. Br J Clin Pharmacol. 2014 Sep;78(3):543-55. doi: 10.1111/bcp.12378.

Contoh Produk & Brand

Produk: 20 • International brands: 0
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