Peringatan Keamanan

There is limited information in the literature regarding an overdose with ripretinib, and LD50 information is not readily available.L13769 Like other kinase inhibitors, an overdose with ripretinib likely results in hematological toxicity, skin toxicity, as well as muscle, liver, and gastrointestinal toxicity.A203156,L13769

Ripretinib

DB14840

small molecule approved

Deskripsi

Ripretinib is a kinase inhibitor used for the treatment of advanced gastrointestinal stromal tumor (GIST) that has not adequately responded to other kinase inhibitors such as sunitinib and imatinib. Ripretinib, also known as Qinlock, is manufactured by Deciphera Pharmaceuticals and was initially approved by the FDA on May 15, 2020.L13769

It is the first drug approved as a fourth-line therapy in the specific setting of prior treatment with a minimum of 3 other kinase inhibitors.L13778

Struktur Molekul 2D

Berat 510.367
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The average half-life of ripretinib is 14.8 hours.[L13769]
Volume Distribusi The mean volume of distribution of ripretinib is 307 L.[L13769]
Klirens (Clearance) The mean apparent clearance of ripretinib is 15.3 L/hour.[L13769]

Absorpsi

Ripretinib is absorbed in the gastrointestinal tract and Tmax is achieved in 4 hours, with steady-state concentrations reached within 14 days.L13769

Metabolisme

Ripretinib is metabolized by the CYP3A subfamily of enzymes with contributions from CYP2D6 and CYP2E1 to its active metabolite, DP-5439.L13769

Rute Eliminasi

Ripretinib is 34% excreted in the feces and 0.2% excreted in the urine.L13769

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

456 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Ripretinib.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Ripretinib.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Ripretinib.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Ripretinib.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Ripretinib.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Ripretinib.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Ripretinib.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Ripretinib.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Ripretinib.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Ripretinib.
Silodosin The excretion of Silodosin can be decreased when combined with Ripretinib.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Ripretinib.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Ripretinib.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Ripretinib.
Vincristine The excretion of Vincristine can be decreased when combined with Ripretinib.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Ripretinib.
Betrixaban The serum concentration of Betrixaban can be increased when it is combined with Ripretinib.
Vemurafenib The serum concentration of Ripretinib can be increased when it is combined with Vemurafenib.
Pitolisant The serum concentration of Ripretinib can be decreased when it is combined with Pitolisant.
Isavuconazole The serum concentration of Ripretinib can be increased when it is combined with Isavuconazole.
Isavuconazonium The serum concentration of Ripretinib can be increased when it is combined with Isavuconazonium.
Pravastatin Pravastatin may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Caffeine Caffeine may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Pantoprazole Pantoprazole may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Diethylstilbestrol Diethylstilbestrol may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Gefitinib Gefitinib may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Beclomethasone dipropionate Beclomethasone dipropionate may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Progesterone Progesterone may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Sorafenib The serum concentration of Ripretinib can be increased when it is combined with Sorafenib.
Lansoprazole Lansoprazole may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Erlotinib Erlotinib may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Imatinib Imatinib may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Estradiol Estradiol may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Buprenorphine Buprenorphine may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Telmisartan Telmisartan may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Novobiocin Novobiocin may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Hesperetin Hesperetin may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Rabeprazole Rabeprazole may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Sunitinib Sunitinib may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Genistein Genistein may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Topiroxostat Topiroxostat may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Daidzin Daidzin may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Fusidic acid The metabolism of Ripretinib can be decreased when combined with Fusidic acid.
Naringenin Naringenin may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Quercetin Quercetin may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Taurocholic acid Taurocholic acid may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Elacridar Elacridar may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Vandetanib Vandetanib may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Dovitinib Dovitinib may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Eltrombopag Eltrombopag may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Simeprevir The metabolism of Ripretinib can be decreased when combined with Simeprevir.
Safinamide Safinamide may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Vismodegib Vismodegib may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Rilpivirine Rilpivirine may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Teriflunomide Teriflunomide may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Ponatinib Ponatinib may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Cannabidiol Cannabidiol may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Palbociclib Palbociclib may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Daclatasvir Daclatasvir may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Dasabuvir Dasabuvir may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Rolapitant Rolapitant may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Paritaprevir Paritaprevir may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Alectinib Alectinib may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Velpatasvir Velpatasvir may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Istradefylline Istradefylline may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Glasdegib Glasdegib may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Fostamatinib Fostamatinib may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Voxilaprevir Voxilaprevir may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Gilteritinib Gilteritinib may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Brigatinib Brigatinib may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Rucaparib Rucaparib may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Fedratinib The serum concentration of Ripretinib can be increased when it is combined with Fedratinib.
Enasidenib Enasidenib may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Pibrentasvir Pibrentasvir may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Glecaprevir Glecaprevir may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Estradiol acetate Estradiol acetate may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Estradiol benzoate Estradiol benzoate may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Estradiol cypionate Estradiol cypionate may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Estradiol dienanthate Estradiol dienanthate may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Estradiol valerate Estradiol valerate may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Nabiximols Nabiximols may decrease the excretion rate of Ripretinib which could result in a higher serum level.
Folic acid Ripretinib may decrease the excretion rate of Folic acid which could result in a higher serum level.
Conjugated estrogens Ripretinib may decrease the excretion rate of Conjugated estrogens which could result in a higher serum level.
Allopurinol Ripretinib may decrease the excretion rate of Allopurinol which could result in a higher serum level.
Cerivastatin Ripretinib may decrease the excretion rate of Cerivastatin which could result in a higher serum level.
Teniposide Ripretinib may decrease the excretion rate of Teniposide which could result in a higher serum level.
Prazosin Ripretinib may decrease the excretion rate of Prazosin which could result in a higher serum level.
Raloxifene Ripretinib may decrease the excretion rate of Raloxifene which could result in a higher serum level.
Celecoxib Ripretinib may decrease the excretion rate of Celecoxib which could result in a higher serum level.
Zidovudine Ripretinib may decrease the excretion rate of Zidovudine which could result in a higher serum level.
Oxaliplatin Ripretinib may decrease the excretion rate of Oxaliplatin which could result in a higher serum level.
Fluorouracil Ripretinib may decrease the excretion rate of Fluorouracil which could result in a higher serum level.
Methotrexate Ripretinib may decrease the excretion rate of Methotrexate which could result in a higher serum level.
Ivermectin Ripretinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Testosterone Ripretinib may decrease the excretion rate of Testosterone which could result in a higher serum level.
Clofarabine Ripretinib may decrease the excretion rate of Clofarabine which could result in a higher serum level.
Sumatriptan Ripretinib may decrease the excretion rate of Sumatriptan which could result in a higher serum level.
Tamoxifen Ripretinib may decrease the excretion rate of Tamoxifen which could result in a higher serum level.
Mycophenolate mofetil Ripretinib may decrease the excretion rate of Mycophenolate mofetil which could result in a higher serum level.

Target Protein

Mast/stem cell growth factor receptor Kit KIT
Platelet-derived growth factor receptor beta PDGFRB
Angiopoietin-1 receptor TEK
Vascular endothelial growth factor receptor 2 KDR
Serine/threonine-protein kinase B-raf BRAF
Platelet-derived growth factor receptor alpha PDGFRA

Referensi & Sumber

Artikel (PubMed)
  • PMID: 31755321
    Nemunaitis J, Bauer S, Blay JY, Choucair K, Gelderblom H, George S, Schoffski P, Mehren MV, Zalcberg J, Achour H, Ruiz-Soto R, Heinrich MC: Intrigue: Phase III study of ripretinib versus sunitinib in advanced gastrointestinal stromal tumor after imatinib. Future Oncol. 2020 Jan;16(1):4251-4264. doi: 10.2217/fon-2019-0633. Epub 2019 Nov 22.
  • PMID: 31205499
    Mazzocca A, Napolitano A, Silletta M, Spalato Ceruso M, Santini D, Tonini G, Vincenzi B: New frontiers in the medical management of gastrointestinal stromal tumours. Ther Adv Med Oncol. 2019 May 17;11:1758835919841946. doi: 10.1177/1758835919841946. eCollection 2019.
  • PMID: 31267077
    Villanueva MT: Ripretinib turns off the switch in GIST. Nat Rev Drug Discov. 2019 Jul;18(7):499. doi: 10.1038/d41573-019-00099-4.
  • PMID: 30259761
    Kannaiyan R, Mahadevan D: A comprehensive review of protein kinase inhibitors for cancer therapy. Expert Rev Anticancer Ther. 2018 Dec;18(12):1249-1270. doi: 10.1080/14737140.2018.1527688. Epub 2018 Oct 9.
  • PMID: 32273716
    Liu P, Tan F, Liu H, Li B, Lei T, Zhao X: The Use of Molecular Subtypes for Precision Therapy of Recurrent and Metastatic Gastrointestinal Stromal Tumor. Onco Targets Ther. 2020 Mar 24;13:2433-2447. doi: 10.2147/OTT.S241331. eCollection 2020.
  • PMID: 26826719
    Kozuki T: Skin problems and EGFR-tyrosine kinase inhibitor. Jpn J Clin Oncol. 2016 Apr;46(4):291-8. doi: 10.1093/jjco/hyv207. Epub 2016 Jan 29.

Contoh Produk & Brand

Produk: 4 • International brands: 0
Produk
  • Qinlock
    Tablet • 50 mg • Oral • EU • Approved
  • Qinlock
    Tablet • 50 mg • Oral • EU • Approved
  • Qinlock
    Tablet • 50 mg • Oral • Canada • Approved
  • Qinlock
    Tablet • 50 mg/1 • Oral • US • Approved

Sekuens Gen/Protein (FASTA)

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