Peringatan Keamanan

The most common adverse reactions (>5%) associated with alectinib use were fatigue, constipation, edema, and myalgia. Less common effects associated with use were hepatotoxicity, interstitial lung disease (ILD)/pneumonitis, bradycardia, severe myalgia and creatine phosphokinase (CPK) elevation, and embryo-fetal toxicity. Females of reproductive potential are advised to use effective contraception during treatment with alectinib and for 1 week following the final dose.

Alectinib

DB11363

small molecule approved investigational

Deskripsi

Alectinib is a second generation oral drug that selectively inhibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase. It is specifically used in the treatment of non-small cell lung cancer (NSCLC) expressing the ALK-EML4 (echinoderm microtubule-associated protein-like 4) fusion protein that causes proliferation of NSCLC cells. Inhibition of ALK prevents phosphorylation and subsequent downstream activation of STAT3 and AKT resulting in reduced tumour cell viability.

Approved under accelerated approval in 2015, alectinib is indicated for use in patients who have progressed on or were not tolerant of crizotinib, which is associated with the development of resistance.

Struktur Molekul 2D

Berat 482.6166
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 elimination half life is 33 hr for alectinib and 31 hr for M4.
Volume Distribusi 4016 L
Klirens (Clearance) The apparent clearance is 81.9L/hr for alectinib and 217 L/hr for M4.

Absorpsi

Alectinib reached maximal concentrations at 4 hours following administration of 600 mg twice daily under fed conditions in patients with ALK-positive NSCLC. The absolute bioavailability was 37% in the fed state. A high-fat, high-calorie meal increased the combined exposure of alectinib and its major metabolite M4 by 3.1-fold following oral administration of a single 600 mg dose.

Metabolisme

Alectinib is metabolized by CYP3A4 to its major active metabolite M4. M4 is then further metabolized by CYP3A4. Both alectinib and M4 demonstrate similar in vivo and in vitro activity. In vitro studies suggest that alectinib is not a substrate for P-gp while M4 is.

Rute Eliminasi

When radioactively labeled, 98% of radioactivity was found in feces with 84% of that amount excreted as unchanged alectinib and 6% as M4. Less than 0.5% was found to be recovered in urine.

Interaksi Makanan

3 Data
  • 1. Exercise caution with grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of alectinib.
  • 2. Exercise caution with St. John's Wort. This herb induces CYP3A metabolism, which may reduce serum levels of alectinib.
  • 3. Take with food.

Interaksi Obat

559 Data
Modafinil The metabolism of Alectinib can be increased when combined with Modafinil.
Armodafinil The metabolism of Alectinib can be increased when combined with Armodafinil.
Metreleptin The metabolism of Alectinib can be increased when combined with Metreleptin.
Propacetamol The serum concentration of Propacetamol can be increased when it is combined with Alectinib.
Crizotinib The metabolism of Alectinib can be decreased when combined with Crizotinib.
Folic acid Alectinib may decrease the excretion rate of Folic acid which could result in a higher serum level.
Allopurinol Alectinib may decrease the excretion rate of Allopurinol which could result in a higher serum level.
Celecoxib Alectinib may decrease the excretion rate of Celecoxib which could result in a higher serum level.
Oxaliplatin Alectinib may decrease the excretion rate of Oxaliplatin which could result in a higher serum level.
Fluorouracil Alectinib may decrease the excretion rate of Fluorouracil which could result in a higher serum level.
Clofarabine Alectinib may decrease the excretion rate of Clofarabine which could result in a higher serum level.
Nitrofurantoin Alectinib may decrease the excretion rate of Nitrofurantoin which could result in a higher serum level.
Riluzole Alectinib may decrease the excretion rate of Riluzole which could result in a higher serum level.
Sulfasalazine Alectinib may decrease the excretion rate of Sulfasalazine which could result in a higher serum level.
Tegaserod Alectinib may decrease the excretion rate of Tegaserod which could result in a higher serum level.
Leflunomide Alectinib may decrease the excretion rate of Leflunomide which could result in a higher serum level.
Alvocidib Alectinib may decrease the excretion rate of Alvocidib which could result in a higher serum level.
Teriflunomide Alectinib may decrease the excretion rate of Teriflunomide which could result in a higher serum level.
Riociguat Alectinib may decrease the excretion rate of Riociguat which could result in a higher serum level.
Fimasartan Alectinib may decrease the excretion rate of Fimasartan which could result in a higher serum level.
Revefenacin Alectinib may decrease the excretion rate of Revefenacin which could result in a higher serum level.
Delafloxacin Alectinib may decrease the excretion rate of Delafloxacin which could result in a higher serum level.
Glasdegib Alectinib may decrease the excretion rate of Glasdegib which could result in a higher serum level.
Darolutamide Alectinib may decrease the excretion rate of Darolutamide which could result in a higher serum level.
Vincristine Alectinib may decrease the excretion rate of Vincristine which could result in a higher serum level.
Afatinib Alectinib may decrease the excretion rate of Afatinib which could result in a higher serum level.
Pravastatin Alectinib may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Conjugated estrogens Alectinib may decrease the excretion rate of Conjugated estrogens which could result in a higher serum level.
Prazosin Alectinib may decrease the excretion rate of Prazosin which could result in a higher serum level.
Zidovudine Alectinib may decrease the excretion rate of Zidovudine which could result in a higher serum level.
Methotrexate Alectinib may decrease the excretion rate of Methotrexate which could result in a higher serum level.
Sumatriptan Alectinib may decrease the excretion rate of Sumatriptan which could result in a higher serum level.
Mycophenolate mofetil Alectinib may decrease the excretion rate of Mycophenolate mofetil which could result in a higher serum level.
Lamivudine Alectinib may decrease the excretion rate of Lamivudine which could result in a higher serum level.
Irinotecan Alectinib may decrease the excretion rate of Irinotecan which could result in a higher serum level.
Donepezil Alectinib may decrease the excretion rate of Donepezil which could result in a higher serum level.
Dactinomycin Alectinib may decrease the excretion rate of Dactinomycin which could result in a higher serum level.
Ezetimibe Alectinib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Camptothecin Alectinib may decrease the excretion rate of Camptothecin which could result in a higher serum level.
Rivaroxaban Alectinib may decrease the excretion rate of Rivaroxaban which could result in a higher serum level.
Apixaban Alectinib may decrease the excretion rate of Apixaban which could result in a higher serum level.
Ponatinib Alectinib may decrease the excretion rate of Ponatinib which could result in a higher serum level.
Dolutegravir Alectinib may decrease the excretion rate of Dolutegravir which could result in a higher serum level.
Sofosbuvir Alectinib may decrease the excretion rate of Sofosbuvir which could result in a higher serum level.
Ombitasvir Alectinib may decrease the excretion rate of Ombitasvir which could result in a higher serum level.
Velpatasvir Alectinib may decrease the excretion rate of Velpatasvir which could result in a higher serum level.
Talazoparib The serum concentration of Talazoparib can be increased when it is combined with Alectinib.
Abemaciclib Alectinib may decrease the excretion rate of Abemaciclib which could result in a higher serum level.
Voxilaprevir Alectinib may decrease the excretion rate of Voxilaprevir which could result in a higher serum level.
Copanlisib Alectinib may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Lusutrombopag Alectinib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level.
Pibrentasvir Alectinib may decrease the excretion rate of Pibrentasvir which could result in a higher serum level.
Tucatinib Alectinib may decrease the excretion rate of Tucatinib which could result in a higher serum level.
Selumetinib Alectinib may decrease the excretion rate of Selumetinib which could result in a higher serum level.
Pralatrexate Alectinib may decrease the excretion rate of Pralatrexate which could result in a higher serum level.
Ripretinib Alectinib may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Fostemsavir Alectinib may decrease the excretion rate of Fostemsavir which could result in a higher serum level.
Topotecan Alectinib may decrease the excretion rate of Topotecan which could result in a higher serum level.
Brigatinib Alectinib may decrease the excretion rate of Brigatinib which could result in a higher serum level.
Testosterone cypionate Alectinib may decrease the excretion rate of Testosterone cypionate which could result in a higher serum level.
Testosterone enanthate Alectinib may decrease the excretion rate of Testosterone enanthate which could result in a higher serum level.
Ivermectin Alectinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Mitoxantrone Alectinib may decrease the excretion rate of Mitoxantrone which could result in a higher serum level.
Lenvatinib Alectinib may decrease the excretion rate of Lenvatinib which could result in a higher serum level.
Gefitinib Alectinib may decrease the excretion rate of Gefitinib which could result in a higher serum level.
Etoposide Alectinib may decrease the excretion rate of Etoposide which could result in a higher serum level.
Trilaciclib Alectinib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Bexarotene The metabolism of Alectinib can be increased when combined with Bexarotene.
Bosentan The metabolism of Alectinib can be increased when combined with Bosentan.
Nafcillin The metabolism of Alectinib can be increased when combined with Nafcillin.
Efavirenz The metabolism of Alectinib can be decreased when combined with Efavirenz.
Etravirine The metabolism of Alectinib can be increased when combined with Etravirine.
Avasimibe The metabolism of Alectinib can be increased when combined with Avasimibe.
Echinacea The metabolism of Alectinib can be increased when combined with Echinacea.
Dexamethasone acetate The metabolism of Alectinib can be increased when combined with Dexamethasone acetate.
Topiramate The metabolism of Alectinib can be increased when combined with Topiramate.
Rifabutin The metabolism of Alectinib can be increased when combined with Rifabutin.
Warfarin The metabolism of Alectinib can be increased when combined with Warfarin.
Felbamate The metabolism of Alectinib can be increased when combined with Felbamate.
Genistein The metabolism of Alectinib can be increased when combined with Genistein.
Oritavancin The metabolism of Alectinib can be increased when combined with Oritavancin.
Rufinamide The metabolism of Alectinib can be increased when combined with Rufinamide.
Glycerol phenylbutyrate The metabolism of Alectinib can be increased when combined with Glycerol phenylbutyrate.
Eslicarbazepine acetate The metabolism of Alectinib can be increased when combined with Eslicarbazepine acetate.
Lesinurad The metabolism of Alectinib can be increased when combined with Lesinurad.
Asunaprevir The metabolism of Alectinib can be increased when combined with Asunaprevir.
Pitolisant The metabolism of Alectinib can be increased when combined with Pitolisant.
Sarilumab The metabolism of Alectinib can be increased when combined with Sarilumab.
Esketamine The metabolism of Alectinib can be increased when combined with Esketamine.
Isavuconazole The metabolism of Alectinib can be increased when combined with Isavuconazole.
Acetaminophen The metabolism of Alectinib can be increased when combined with Acetaminophen.
Testosterone The metabolism of Alectinib can be increased when combined with Testosterone.
Enasidenib The metabolism of Alectinib can be increased when combined with Enasidenib.
Cerivastatin The metabolism of Alectinib can be increased when combined with Cerivastatin.
Tamoxifen The metabolism of Alectinib can be increased when combined with Tamoxifen.
Vemurafenib The metabolism of Alectinib can be increased when combined with Vemurafenib.
Calcitriol The metabolism of Alectinib can be increased when combined with Calcitriol.
Vitamin E The metabolism of Alectinib can be increased when combined with Vitamin E.
Flunisolide The metabolism of Alectinib can be increased when combined with Flunisolide.
Troglitazone The metabolism of Alectinib can be increased when combined with Troglitazone.

Target Protein

ALK tyrosine kinase receptor ALK

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25428710
    McKeage K: Alectinib: a review of its use in advanced ALK-rearranged non-small cell lung cancer. Drugs. 2015 Jan;75(1):75-82. doi: 10.1007/s40265-014-0329-y.
  • PMID: 21575866
    Sakamoto H, Tsukaguchi T, Hiroshima S, Kodama T, Kobayashi T, Fukami TA, Oikawa N, Tsukuda T, Ishii N, Aoki Y: CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011 May 17;19(5):679-90. doi: 10.1016/j.ccr.2011.04.004.
  • PMID: 24887559
    Kodama T, Tsukaguchi T, Yoshida M, Kondoh O, Sakamoto H: Selective ALK inhibitor alectinib with potent antitumor activity in models of crizotinib resistance. Cancer Lett. 2014 Sep 1;351(2):215-21. doi: 10.1016/j.canlet.2014.05.020. Epub 2014 Jun 2.
  • PMID: 26753004
    Sullivan I, Planchard D: ALK inhibitors in non-small cell lung cancer: the latest evidence and developments. Ther Adv Med Oncol. 2016 Jan;8(1):32-47. doi: 10.1177/1758834015617355.

Contoh Produk & Brand

Produk: 4 • International brands: 1
Produk
  • Alecensa
    Capsule • 150 mg/1 • Oral • US • Approved
  • Alecensa
    Capsule • 150 mg • Oral • EU • Approved
  • Alecensa
    Capsule • 150 mg • Oral • EU • Approved
  • Alecensaro
    Capsule • 150 mg • Oral • Canada • Approved
International Brands
  • Alecensa

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