Peringatan Keamanan

Carcinogenic studies have not been performed and duvelisib did not produce any genetic damage in vitro or in vivo. In the case of fertility studies, there was found some histological abnormalities in male and female rats such as seminiferous epithelial atrophy, decreased testes weight, soft testes, small epididymis, oligo/aspermia, decreased ovary weight, and uterine atrophy.FDA label

Duvelisib

DB11952

small molecule approved investigational

Deskripsi

Duvelisib, also known as IPI-145 and INK-1197, is a small-molecule inhibitor of phosphoinositide-3 kinases that was designed initially to prove that simultaneous inhibition of the isoforms delta and gamma can produce a broad adaptative and innate immune cell inhibitory activity. All the work around duvelisib showed that this agent is a potent inhibitor of both forms.A39025 Duvelisib was developed by Verastem, Inc and FDA approved on September 24, 2018.L4585

Struktur Molekul 2D

Berat 416.87
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The reported half-life of duvelisib is in the range of 5.2 to 10.9 hours.[A39035]
Volume Distribusi The volume of distribution of duvelisib ranges from 26 to 102 L.[A39035]
Klirens (Clearance) Duvelisib clearance rate is reported to be in the range of 3.6 to 11.2 L/h.[A39035]

Absorpsi

Duvelisib is rapidly absorbed and its peak plasma concentration is reached 1-2 hours after initial administration with a bioavailability of 42% and with a minimal accumulation whose rate ranges between 1.5 and 2.9.A39034 The maximal plasma concentration is reported to range in between 471 to 3294 ng/ml with a systemic exposure ranging from 2001 to 19059 ng.h/ml. Changes in the administered dose produce correspondent changes in all absorption parameters indicating a dose-response profile.A39035

Metabolisme

Duvelesib is mainly metabolized by CYP3A4.FDA label

Rute Eliminasi

Duvelisib is eliminated after 3.5-9.5 hours when administered as a single dose and after 6.5-11.7 hours when given in multiple doses.A39034 From the administered dose, 79% os excreted in feces and 14% in urine. About 10% of the total administered dose is secreted unchanged.FDA label

Interaksi Makanan

2 Data
  • 1. Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of duvelisib.
  • 2. Take with or without food.

Interaksi Obat

667 Data
Ranolazine The serum concentration of Duvelisib can be increased when it is combined with Ranolazine.
Phenytoin The metabolism of Duvelisib can be increased when combined with Phenytoin.
Fosphenytoin The metabolism of Duvelisib can be increased when combined with Fosphenytoin.
Lumacaftor The serum concentration of Duvelisib can be decreased when it is combined with Lumacaftor.
Bexarotene The metabolism of Duvelisib can be increased when combined with Bexarotene.
Bosentan The metabolism of Duvelisib can be increased when combined with Bosentan.
Nafcillin The metabolism of Duvelisib can be increased when combined with Nafcillin.
Modafinil The metabolism of Duvelisib can be increased when combined with Modafinil.
Etravirine The metabolism of Duvelisib can be increased when combined with Etravirine.
Avasimibe The metabolism of Duvelisib can be increased when combined with Avasimibe.
Echinacea The metabolism of Duvelisib can be increased when combined with Echinacea.
Dexamethasone acetate The metabolism of Duvelisib can be increased when combined with Dexamethasone acetate.
Vemurafenib The serum concentration of Duvelisib can be increased when it is combined with Vemurafenib.
Apalutamide The serum concentration of Duvelisib can be decreased when it is combined with Apalutamide.
Pitolisant The serum concentration of Duvelisib can be decreased when it is combined with Pitolisant.
Isavuconazole The serum concentration of Duvelisib can be increased when it is combined with Isavuconazole.
Isavuconazonium The serum concentration of Duvelisib can be increased when it is combined with Isavuconazonium.
Pravastatin Pravastatin may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Diethylstilbestrol Diethylstilbestrol may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Estradiol Estradiol may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Novobiocin Novobiocin may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Hesperetin Hesperetin may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Rabeprazole Rabeprazole may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Topiroxostat Topiroxostat may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Daidzin Daidzin may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Fusidic acid The metabolism of Duvelisib can be decreased when combined with Fusidic acid.
Naringenin Naringenin may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Eltrombopag Eltrombopag may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Simeprevir The metabolism of Duvelisib can be decreased when combined with Simeprevir.
Safinamide Safinamide may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Vismodegib Vismodegib may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Teriflunomide Teriflunomide may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Cannabidiol Cannabidiol may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Dasabuvir Dasabuvir may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Glasdegib Glasdegib may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Fostamatinib Fostamatinib may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Gilteritinib Gilteritinib may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Estradiol acetate Estradiol acetate may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Estradiol benzoate Estradiol benzoate may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Estradiol cypionate Estradiol cypionate may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Estradiol dienanthate Estradiol dienanthate may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Estradiol valerate Estradiol valerate may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Medical Cannabis The metabolism of Duvelisib can be decreased when combined with Medical Cannabis.
Nabiximols Nabiximols may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Fedratinib The serum concentration of Duvelisib can be increased when it is combined with Fedratinib.
Istradefylline Istradefylline may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Caffeine Caffeine may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Pantoprazole Pantoprazole may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Gefitinib Gefitinib may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Progesterone Progesterone may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Lansoprazole Lansoprazole may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Buprenorphine Buprenorphine may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Telmisartan Telmisartan may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Genistein Genistein may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Quercetin Quercetin may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Letermovir The metabolism of Duvelisib can be decreased when combined with Letermovir.
Taurocholic acid Taurocholic acid may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Dovitinib Dovitinib may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Paritaprevir Paritaprevir may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Rilpivirine Rilpivirine may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Ripretinib Ripretinib may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Fostemsavir Fostemsavir may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Pralsetinib Pralsetinib may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Avanafil The serum concentration of Avanafil can be increased when it is combined with Duvelisib.
Tivozanib Tivozanib may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Belumosudil Belumosudil may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Fluconazole The metabolism of Duvelisib can be decreased when combined with Fluconazole.
Erythromycin The serum concentration of Duvelisib can be increased when it is combined with Erythromycin.
Reserpine The serum concentration of Duvelisib can be increased when it is combined with Reserpine.
Loxapine The serum concentration of Duvelisib can be increased when it is combined with Loxapine.
Quinine The serum concentration of Duvelisib can be increased when it is combined with Quinine.
Toremifene The serum concentration of Duvelisib can be increased when it is combined with Toremifene.
Mifepristone The serum concentration of Duvelisib can be increased when it is combined with Mifepristone.
Zonisamide The serum concentration of Duvelisib can be increased when it is combined with Zonisamide.
Carvedilol The serum concentration of Duvelisib can be increased when it is combined with Carvedilol.
Propafenone The serum concentration of Duvelisib can be increased when it is combined with Propafenone.
Lapatinib The serum concentration of Duvelisib can be increased when it is combined with Lapatinib.
Paliperidone The serum concentration of Duvelisib can be increased when it is combined with Paliperidone.
Mibefradil The serum concentration of Duvelisib can be increased when it is combined with Mibefradil.
Biricodar The serum concentration of Duvelisib can be increased when it is combined with Biricodar.
Elacridar Elacridar may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Flibanserin The serum concentration of Duvelisib can be increased when it is combined with Flibanserin.
Zosuquidar The serum concentration of Duvelisib can be increased when it is combined with Zosuquidar.
Tariquidar The serum concentration of Duvelisib can be increased when it is combined with Tariquidar.
Brefeldin A The serum concentration of Duvelisib can be increased when it is combined with Brefeldin A.
Ivacaftor The serum concentration of Duvelisib can be increased when it is combined with Ivacaftor.
Linagliptin The metabolism of Duvelisib can be decreased when combined with Linagliptin.
Canagliflozin The serum concentration of Duvelisib can be increased when it is combined with Canagliflozin.
Afatinib Afatinib may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Ledipasvir Ledipasvir may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Vorapaxar The serum concentration of Duvelisib can be increased when it is combined with Vorapaxar.
Suvorexant The serum concentration of Duvelisib can be increased when it is combined with Suvorexant.
Netupitant The metabolism of Duvelisib can be decreased when combined with Netupitant.
Daclatasvir Daclatasvir may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Niguldipine The serum concentration of Duvelisib can be increased when it is combined with Niguldipine.
Rolapitant Rolapitant may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Asunaprevir The serum concentration of Duvelisib can be increased when it is combined with Asunaprevir.
Velpatasvir Velpatasvir may decrease the excretion rate of Duvelisib which could result in a higher serum level.
Valspodar The serum concentration of Duvelisib can be increased when it is combined with Valspodar.

Target Protein

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform PIK3CG
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform PIK3CD

Referensi & Sumber

Artikel (PubMed)
  • PMID: 24211136
    Winkler DG, Faia KL, DiNitto JP, Ali JA, White KF, Brophy EE, Pink MM, Proctor JL, Lussier J, Martin CM, Hoyt JG, Tillotson B, Murphy EL, Lim AR, Thomas BD, Macdougall JR, Ren P, Liu Y, Li LS, Jessen KA, Fritz CC, Dunbar JL, Porter JR, Rommel C, Palombella VJ, Changelian PS, Kutok JL: PI3K-delta and PI3K-gamma inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74. doi: 10.1016/j.chembiol.2013.09.017. Epub 2013 Nov 7.
  • PMID: 24501284
    Authors unspecified: IPI-145 shows promise in CLL patients. Cancer Discov. 2014 Feb;4(2):136. doi: 10.1158/2159-8290.CD-NB2013-177. Epub 2013 Dec 12.
  • PMID: 24244039
    Boyle DL, Kim HR, Topolewski K, Bartok B, Firestein GS: Novel phosphoinositide 3-kinase delta,gamma inhibitor: potent anti-inflammatory effects and joint protection in models of rheumatoid arthritis. J Pharmacol Exp Ther. 2014 Feb;348(2):271-80. doi: 10.1124/jpet.113.205955. Epub 2013 Nov 15.
  • PMID: 28945111
    Lampson BL, Brown JR: PI3Kdelta-selective and PI3Kalpha/delta-combinatorial inhibitors in clinical development for B-cell non-Hodgkin lymphoma. Expert Opin Investig Drugs. 2017 Nov;26(11):1267-1279. doi: 10.1080/13543784.2017.1384815. Epub 2017 Oct 6.
  • PMID: 28388280
    Vangapandu HV, Jain N, Gandhi V: Duvelisib: a phosphoinositide-3 kinase delta/gamma inhibitor for chronic lymphocytic leukemia. Expert Opin Investig Drugs. 2017 May;26(5):625-632. doi: 10.1080/13543784.2017.1312338. Epub 2017 Apr 13.
  • PMID: 29191916
    Flinn IW, O'Brien S, Kahl B, Patel M, Oki Y, Foss FF, Porcu P, Jones J, Burger JA, Jain N, Kelly VM, Allen K, Douglas M, Sweeney J, Kelly P, Horwitz S: Duvelisib, a novel oral dual inhibitor of PI3K-delta,gamma, is clinically active in advanced hematologic malignancies. Blood. 2018 Feb 22;131(8):877-887. doi: 10.1182/blood-2017-05-786566. Epub 2017 Nov 30.

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