Ribociclib

DB11730

small molecule approved investigational

Deskripsi

Ribociclib is a selective cyclin-dependent kinase inhibitor, a class of drugs that help slow the progression of cancer by inhibiting two proteins called cyclin-dependent kinase 4 and 6 (CDK4/6). These proteins, when over-activated, can enable cancer cells to grow and divide too quickly.

Ribociclib was approved by the FDA in March 2017 under the brand name Kisqali.

Struktur Molekul 2D

Berat 434.548
Wujud -

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) At steady-state in patients with advanced cancer, the mean plasma effective half-life of ribociclib was 32 hours.[L51529] In healthy adults receiving the 600 mg dose, the mean apparent plasma terminal half-life of ribociclib ranged from 29.7 to 54.7 hours and mean apparent oral clearance of ribociclib ranged from 39.9 to 77.5 L/h.[L51529]
Volume Distribusi At steady-state, the apparent volume of distribution of ribociclib was 1090 L.[L51529]
Klirens (Clearance) At steady-state in patients with advanced cancer administered receiving the 600 mg dose, the mean apparent oral clearance of ribociclib was 25.5 L/h.[L51529] At steady-state in patients with early breast cancer administered receiving the 400 mg dose, the mean apparent oral clearance of ribociclib was 38.4 L/h.[L51529]

Absorpsi

The mean absolute bioavailability of ribociclib after a single oral dose of 600 mg was 65.8%.L51529 Following repeated 600 mg once daily administration, steady-state was generally achieved after 8 days and the mean steady-state Cmax and AUC were 1820 ng/mL and 23800 ng*h/mL, respectively.L51529 The Tmax of ribociclib at steady-state generally occurs between 1 and 4 hours following administration.L51529

Metabolisme

Ribociclib undergoes extensive hepatic metabolism, primarily via oxidative reactions mediated by CYP3A4.L51529 Major circulating metabolites following oral administration include metabolite M13 (CCI284, N-hydroxylation), M4 (LEQ803, N-demethylation), and M1 (secondary glucuronide), each representing an estimated 9%, 9%, and 8% of total radioactivity, and 22%, 20%, and 18% of ribociclib exposure.L51529 Parent drug is the major circulating entity in plasma, accounting for 44% of total exposure.L51529

Rute Eliminasi

Unchanged parent drug accounts for only 17% and 12% of the administered dose excreted in feces and urine, respectively.L51529 Metabolite M4 (LEQ803) represented approximately 14% and 4% of the administered dose in feces and urine, respectively.L51529

Interaksi Makanan

4 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits CYP3A metabolism, which may increase the serum concentration of ribociclib.
  • 2. Avoid St. John's Wort. This herb induces CYP3A metabolism, which may reduce serum levels of ribociclib.
  • 3. Take at the same time every day. Official labeling suggests taking ribociclib in the morning.
  • 4. Take with or without food.

Interaksi Obat

1159 Data
Armodafinil The metabolism of Ribociclib can be increased when combined with Armodafinil.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Ribociclib.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Ribociclib.
Cilostazol The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Cilostazol.
Colchicine The metabolism of Colchicine can be decreased when combined with Ribociclib.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Ribociclib.
Iloperidone The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Iloperidone.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Ribociclib.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Ribociclib.
Vardenafil The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Vardenafil.
Metreleptin The metabolism of Ribociclib can be increased when combined with Metreleptin.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Ribociclib.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Ribociclib.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Ribociclib.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Ribociclib.
Tacrolimus The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Tacrolimus.
Crizotinib The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Crizotinib.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Ribociclib.
Leuprolide The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Leuprolide.
Goserelin The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Goserelin.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Moxifloxacin.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Sulfisoxazole.
Sulpiride The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Sulpiride.
Droperidol The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Droperidol.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Oxaliplatin.
Fluorouracil The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Fluorouracil.
Perflutren The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Perflutren.
Atropine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Atropine.
Adenosine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Adenosine.
Pentamidine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Pentamidine.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Gadobenic acid.
Carbinoxamine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Carbinoxamine.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Nalidixic acid.
Cinoxacin The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Cinoxacin.
Levosimendan The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Levosimendan.
Mesoridazine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Mesoridazine.
Desloratadine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Desloratadine.
Lomefloxacin The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Lomefloxacin.
Dimenhydrinate The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Dimenhydrinate.
Papaverine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Papaverine.
Levofloxacin The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Levofloxacin.
Gemifloxacin The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Gemifloxacin.
Ofloxacin The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Ofloxacin.
Flecainide The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Flecainide.
Probucol The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Probucol.
Aceprometazine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Aceprometazine.
Terlipressin The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Terlipressin.
Lofexidine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Lofexidine.
Pracinostat The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Pracinostat.
Technetium Tc-99m ciprofloxacin The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Technetium Tc-99m ciprofloxacin.
Garenoxacin The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Garenoxacin.
Tedisamil The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Tedisamil.
Tucidinostat The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Tucidinostat.
Telavancin The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Telavancin.
Nemonoxacin The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Nemonoxacin.
Antazoline The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Antazoline.
Butriptyline The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Butriptyline.
Lenvatinib The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Lenvatinib.
Melperone The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Melperone.
Amifampridine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Amifampridine.
Mocetinostat The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Mocetinostat.
Entinostat The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Entinostat.
CUDC-101 The risk or severity of QTc prolongation can be increased when Ribociclib is combined with CUDC-101.
Simendan The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Simendan.
Ricolinostat The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Ricolinostat.
Mizolastine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Mizolastine.
Abexinostat The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Abexinostat.
Oxatomide The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Oxatomide.
Sitafloxacin The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Sitafloxacin.
Sultopride The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Sultopride.
Nizofenone The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Nizofenone.
Bunaftine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Bunaftine.
Lorcainide The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Lorcainide.
Dexchlorpheniramine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Dexchlorpheniramine.
Emedastine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Emedastine.
Oxytocin The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Oxytocin.
Esmolol The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Esmolol.
Pregabalin The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Pregabalin.
Benzatropine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Benzatropine.
Atomoxetine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Atomoxetine.
Olanzapine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Olanzapine.
Cetirizine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Cetirizine.
Protriptyline The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Protriptyline.
Buclizine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Buclizine.
Doxylamine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Doxylamine.
Timolol The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Timolol.
Treprostinil The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Treprostinil.
Digoxin The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Digoxin.
Dexbrompheniramine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Dexbrompheniramine.
Hyoscyamine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Hyoscyamine.
Triprolidine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Triprolidine.
Cyproheptadine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Cyproheptadine.
Enoxacin The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Enoxacin.
Pefloxacin The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Pefloxacin.
Foscarnet The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Foscarnet.
Amoxapine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Amoxapine.
Lamotrigine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Lamotrigine.
Amodiaquine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Amodiaquine.
Moricizine The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Moricizine.
Moexipril The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Moexipril.

Target Protein

Cyclin-dependent kinase 4 CDK4
Cyclin-dependent kinase 6 CDK6

Referensi & Sumber

Artikel (PubMed)
  • PMID: 16413469
    Yu Q, Sicinska E, Geng Y, Ahnstrom M, Zagozdzon A, Kong Y, Gardner H, Kiyokawa H, Harris LN, Stal O, Sicinski P: Requirement for CDK4 kinase function in breast cancer. Cancer Cell. 2006 Jan;9(1):23-32.
  • PMID: 24045179
    Rader J, Russell MR, Hart LS, Nakazawa MS, Belcastro LT, Martinez D, Li Y, Carpenter EL, Attiyeh EF, Diskin SJ, Kim S, Parasuraman S, Caponigro G, Schnepp RW, Wood AC, Pawel B, Cole KA, Maris JM: Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82. doi: 10.1158/1078-0432.CCR-13-1675. Epub 2013 Sep 17.
  • PMID: 27542767
    Infante JR, Cassier PA, Gerecitano JF, Witteveen PO, Chugh R, Ribrag V, Chakraborty A, Matano A, Dobson JR, Crystal AS, Parasuraman S, Shapiro GI: A Phase I Study of the Cyclin-Dependent Kinase 4/6 Inhibitor Ribociclib (LEE011) in Patients with Advanced Solid Tumors and Lymphomas. Clin Cancer Res. 2016 Dec 1;22(23):5696-5705. Epub 2016 Aug 19.

Contoh Produk & Brand

Produk: 19 • International brands: 0
Produk
  • Kisqali
    Tablet, film coated • 200 mg/1 • Oral • US • Approved
  • Kisqali
    Tablet, film coated • 200 mg/1 • Oral • US • Approved
  • Kisqali
    Tablet, film coated • 200 mg/1 • Oral • US • Approved
  • Kisqali
    Tablet, film coated • 200 mg • Oral • EU • Approved
  • Kisqali
    Tablet, film coated • 200 mg • Oral • EU • Approved
  • Kisqali
    Tablet, film coated • 200 mg • Oral • EU • Approved
  • Kisqali
    Tablet, film coated • 200 mg • Oral • EU • Approved
  • Kisqali
    Tablet, film coated • 200 mg • Oral • EU • Approved
Menampilkan 8 dari 19 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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