Peringatan Keamanan

Data regarding overdoses of trilaciclib are not readily available.L31828 For grade 3 or worse injection site reactions, acute drug hypersensitivity reactions, and interstitial lung disease; or any other grade 4 toxicities; permanently discontinue trilacilib.L31828

Trilaciclib

DB15442

small molecule approved investigational

Deskripsi

Trilaciclib, or G1T28, is a CDK4 and CDK6 inhibitor, indicated to reduce the incidence of chemotherapy induced myelosuppression in patients before topotecan-containing or platinum and etoposide-containing chemotherapy for extensive stage small cell lung cancer.L31828 CDK4 and CDK6 inhibitors have been investigated since the mid 1990s for their use in tumorigenesis and chemotherapy.A229323 Trilaciclib was first described in the literature in 2016.A229313

Trilaciclib was granted FDA approval on 12 February 2021.L31823

Struktur Molekul 2D

Berat 446.559
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 terminal half life of trilaciblib is approximately 14 h.[L31828]
Volume Distribusi The volume of distribution of trilaciclib at steady state is 1130 L.[L31828]
Klirens (Clearance) The clearance of trilaciclib is 158 L/h.[L31828]

Absorpsi

Cmax and AUC of trilaciclib increase proportionally with dose.A229328,L31828

Metabolisme

Data regarding the metabolism of trilaciclib are not readily available, however it is expected to be extensively metabolised.L31828

Rute Eliminasi

79.1% of a radiolabelled dose is recovered in the feces, 7% as the unchanged parent compound.L31828 14% of a radiolabelled dose is recovered in the urine, 2% as the unchanged parent compound.L31828

Interaksi Obat

474 Data
Ranolazine The serum concentration of Trilaciclib can be increased when it is combined with Ranolazine.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Trilaciclib.
Lumacaftor The serum concentration of Trilaciclib can be decreased when it is combined with Lumacaftor.
Tipiracil The excretion of Tipiracil can be decreased when combined with Trilaciclib.
Vemurafenib The serum concentration of Trilaciclib can be increased when it is combined with Vemurafenib.
Apalutamide The serum concentration of Trilaciclib can be decreased when it is combined with Apalutamide.
Pitolisant The serum concentration of Trilaciclib can be increased when it is combined with Pitolisant.
Isavuconazonium The serum concentration of Trilaciclib can be increased when it is combined with Isavuconazonium.
Isavuconazole The serum concentration of Trilaciclib can be increased when it is combined with Isavuconazole.
Cyclosporine Cyclosporine may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Pravastatin Pravastatin may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Pantoprazole Pantoprazole may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Nelfinavir Nelfinavir may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Diethylstilbestrol Diethylstilbestrol may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Gefitinib Gefitinib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Beclomethasone dipropionate Beclomethasone dipropionate may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Progesterone Progesterone may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Lansoprazole Lansoprazole may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Ritonavir Ritonavir may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Clofazimine Clofazimine may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Buprenorphine Buprenorphine may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Telmisartan Telmisartan may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Novobiocin Novobiocin may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Rabeprazole Rabeprazole may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Saquinavir Saquinavir may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Dexamethasone Dexamethasone may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Sunitinib Sunitinib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Topiroxostat Topiroxostat may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Daidzin Daidzin may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Fusidic acid Fusidic acid may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Naringenin Naringenin may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Quercetin Quercetin may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Taurocholic acid Taurocholic acid may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Nilotinib Nilotinib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Elacridar Elacridar may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Vandetanib Vandetanib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Dovitinib Dovitinib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Simeprevir Simeprevir may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Safinamide Safinamide may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Vismodegib Vismodegib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Rilpivirine Rilpivirine may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Teriflunomide Teriflunomide may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Regorafenib Regorafenib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Ponatinib Ponatinib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Dabrafenib Dabrafenib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Afatinib Afatinib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Cannabidiol Cannabidiol may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Cobicistat Cobicistat may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Palbociclib Palbociclib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Daclatasvir Daclatasvir may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Dasabuvir Dasabuvir may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Rolapitant Rolapitant may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Paritaprevir Paritaprevir may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Alectinib Alectinib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Venetoclax Venetoclax may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Velpatasvir Velpatasvir may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Fostemsavir Fostemsavir may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Dacomitinib Dacomitinib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Glasdegib Glasdegib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Fostamatinib Fostamatinib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Gilteritinib Gilteritinib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Brigatinib Brigatinib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Fedratinib Fedratinib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Darolutamide Darolutamide may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Pibrentasvir Pibrentasvir may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Glecaprevir Glecaprevir may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Nabiximols Nabiximols may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Dexamethasone acetate Dexamethasone acetate may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Ripretinib Ripretinib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Pralsetinib Pralsetinib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Avanafil Avanafil may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Tivozanib Tivozanib may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Belumosudil Belumosudil may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Fluconazole The serum concentration of Trilaciclib can be increased when it is combined with Fluconazole.
Erythromycin The serum concentration of Trilaciclib can be increased when it is combined with Erythromycin.
Sildenafil The serum concentration of Trilaciclib can be increased when it is combined with Sildenafil.
Mefloquine The serum concentration of Trilaciclib can be increased when it is combined with Mefloquine.
Loxapine The serum concentration of Trilaciclib can be increased when it is combined with Loxapine.
Toremifene The serum concentration of Trilaciclib can be increased when it is combined with Toremifene.
Simvastatin The serum concentration of Trilaciclib can be increased when it is combined with Simvastatin.
Mifepristone The serum concentration of Trilaciclib can be increased when it is combined with Mifepristone.
Vardenafil The serum concentration of Trilaciclib can be increased when it is combined with Vardenafil.
Tacrolimus The serum concentration of Trilaciclib can be increased when it is combined with Tacrolimus.
Conivaptan The serum concentration of Trilaciclib can be increased when it is combined with Conivaptan.
Quinidine The serum concentration of Trilaciclib can be increased when it is combined with Quinidine.
Zonisamide The serum concentration of Trilaciclib can be increased when it is combined with Zonisamide.
Tipranavir The serum concentration of Trilaciclib can be increased when it is combined with Tipranavir.
Norgestimate The serum concentration of Trilaciclib can be increased when it is combined with Norgestimate.
Ketoconazole The serum concentration of Trilaciclib can be increased when it is combined with Ketoconazole.
Amiodarone The serum concentration of Trilaciclib can be increased when it is combined with Amiodarone.
Itraconazole Itraconazole may decrease the excretion rate of Trilaciclib which could result in a higher serum level.
Arsenic trioxide The serum concentration of Trilaciclib can be increased when it is combined with Arsenic trioxide.
Clarithromycin The serum concentration of Trilaciclib can be increased when it is combined with Clarithromycin.
Lapatinib The serum concentration of Trilaciclib can be increased when it is combined with Lapatinib.
Paliperidone The serum concentration of Trilaciclib can be increased when it is combined with Paliperidone.
Mibefradil The serum concentration of Trilaciclib can be increased when it is combined with Mibefradil.
Everolimus The serum concentration of Trilaciclib can be increased when it is combined with Everolimus.
Lopinavir The serum concentration of Trilaciclib can be increased when it is combined with Lopinavir.
Ixabepilone The serum concentration of Trilaciclib can be increased when it is combined with Ixabepilone.

Target Protein

Cyclin-dependent kinase 4 CDK4
Cyclin-dependent kinase 6 CDK6
Cyclin-dependent kinase 9 CDK9
Cyclin-dependent kinase 2 CDK2
Cyclin-dependent kinase 5 CDK5
Cyclin-dependent kinase 7 CDK7

Referensi & Sumber

Artikel (PubMed)
  • PMID: 26826116
    Bisi JE, Sorrentino JA, Roberts PJ, Tavares FX, Strum JC: Preclinical Characterization of G1T28: A Novel CDK4/6 Inhibitor for Reduction of Chemotherapy-Induced Myelosuppression. Mol Cancer Ther. 2016 May;15(5):783-93. doi: 10.1158/1535-7163.MCT-15-0775. Epub 2016 Jan 29.
  • PMID: 33004541
    Lai AY, Sorrentino JA, Dragnev KH, Weiss JM, Owonikoko TK, Rytlewski JA, Hood J, Yang Z, Malik RK, Strum JC, Roberts PJ: CDK4/6 inhibition enhances antitumor efficacy of chemotherapy and immune checkpoint inhibitor combinations in preclinical models and enhances T-cell activation in patients with SCLC receiving chemotherapy. J Immunother Cancer. 2020 Oct;8(2). pii: jitc-2020-000847. doi: 10.1136/jitc-2020-000847.
  • PMID: 7883799
    Peters G: The D-type cyclins and their role in tumorigenesis. J Cell Sci Suppl. 1994;18:89-96. doi: 10.1242/jcs.1994.supplement_18.13.
  • PMID: -
    Tiessen RG, Roberts PJ, Sorrentino JA, White HS, Makhuli KM, Bisi JE, Strum JC, van Hoogdalem E, Malik RK: First-in-human Phase 1 safety, PK, and PD study of the CDK4/6 inhibitor G1T28. Journal of Clinical Oncology. 2015 May 20;33(15):2527-2527.

Contoh Produk & Brand

Produk: 1 • International brands: 1
Produk
  • Cosela
    Injection, powder, lyophilized, for solution • 300 mg/20mL • Intravenous • US • Approved
International Brands
  • Cosela — G1 Therapeutics, Inc.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul