Peringatan Keamanan

The LD50 of copanlisib dihydrochloride in male and female rats after a single intravenous dose administration was >23.0 mg/kg, which corresponds to 20.0 mg/kg copanlisib.L48350 There is no information on copanlisib overdose.

Copanlisib

DB12483

small molecule approved investigational

Deskripsi

Copanlisib is a selective pan-Class I phosphoinositide 3-kinase (PI3K) inhibitor with preferential activity against the alpha and delta isoforms. PI3K, a lipid kinase that activates downstream signalling pathways involved in cell survival and growth, that exists in different isoforms and is often overexpressed in hematological malignancies.A261730 Copanlisib was granted accelerated approval by the FDA in September 2017 for the treatment of follicular lymphoma.A261725

Struktur Molekul 2D

Berat 480.529
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The geometric mean terminal elimination half-life of copanlisib is 39.1 (range: 14.6 to 82.4; SD: 15.0) hours.[L48345]
Volume Distribusi The geometric mean volume of distribution is 871 (range: 423 to 2150; SD: 479) L.[L48345]
Klirens (Clearance) The geometric mean clearance is 17.9 (range: 7.3 to 51.4; SD: 8.5) L/hr.[L48345]

Absorpsi

The area under the plasma concentration-time curve (AUC) and maximum plasma concentration (Cmax) of copanlisib increase dose-proportionally over 5 to 93 mg (0.08 to 1.55 times the approved recommended dose) absolute dose range and exhibit linear pharmacokinetics (PK). There is no time-dependency and no accumulation in the pharmacokinetics of copanlisib. The geometric mean (range) steady state copanlisib exposure at 0.8 mg/kg (approximately the approved recommended dose of 60 mg) are 463 (range: 105 to 1670; SD: 584) ng/mL for Cmax and 1570 (range: 536 to 3410; SD: 338) ng x hr/mL for AUC0-25h.L48345

Metabolisme

Copanlisib is primarily metabolized by CYP3A (>90%) and to a lesser extent, CYP1A1 (<10%).A261745, L48345 The M1 metabolite accounts for 5% of total radioactivity in plasma and has a pharmacological activity that is comparable to that of the parent compound.A261745, L48345

Rute Eliminasi

In humans, approximately half of copanlisib is excreted as unchanged parent compound and the other half is excreted as metabolites. Following a single intravenous dose of 12 mg (0.2 times the recommended approved dose) radiolabeled copanlisib, approximately 64% of the administered dose was recovered in feces and 22% in urine within 20 to 34 days. Unchanged copanlisib represented approximately 30% of the administered dose in feces and 15% in urine. Metabolites resulting from CYP450-mediated oxidation accounted for 41% of the administered dose.L48345

Interaksi Makanan

2 Data
  • 1. Avoid grapefruit products. Grapefruit strongly inhibits CYP3A metabolism, which may increase the serum concentration of copanlisib.
  • 2. Avoid St. John's Wort. This herb strongly induces the CYP3A metabolism of copanlisib and may reduce its serum concentration.

Interaksi Obat

644 Data
Modafinil The metabolism of Copanlisib can be increased when combined with Modafinil.
Armodafinil The metabolism of Copanlisib can be increased when combined with Armodafinil.
Ranolazine The metabolism of Copanlisib can be decreased when combined with Ranolazine.
Metreleptin The metabolism of Copanlisib can be increased when combined with Metreleptin.
Crizotinib The metabolism of Copanlisib can be decreased when combined with Crizotinib.
Lumacaftor The metabolism of Copanlisib can be increased when combined with Lumacaftor.
Vemurafenib The metabolism of Copanlisib can be increased when combined with Vemurafenib.
Apalutamide The metabolism of Copanlisib can be increased when combined with Apalutamide.
Pitolisant The serum concentration of Copanlisib can be decreased when it is combined with Pitolisant.
Isavuconazole The metabolism of Copanlisib can be increased when combined with Isavuconazole.
Isavuconazonium The metabolism of Copanlisib can be increased when combined with Isavuconazonium.
Pravastatin Pravastatin may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Novobiocin Novobiocin may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Hesperetin Hesperetin may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Daidzin Daidzin may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Naringenin Naringenin may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Eltrombopag Eltrombopag may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Vismodegib Vismodegib may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Teriflunomide Teriflunomide may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Dasabuvir Dasabuvir may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Caffeine Caffeine may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Darolutamide Darolutamide may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Pantoprazole Pantoprazole may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Telmisartan Telmisartan may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Quercetin Quercetin may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Alectinib Alectinib may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Abemaciclib Abemaciclib may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Taurocholic acid Taurocholic acid may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Fostemsavir Fostemsavir may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Brigatinib Brigatinib may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Lansoprazole Lansoprazole may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Safinamide Safinamide may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Avanafil The serum concentration of Avanafil can be increased when it is combined with Copanlisib.
Rabeprazole Rabeprazole may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Tivozanib Tivozanib may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Cholesterol Cholesterol may increase the excretion rate of Copanlisib which could result in a lower serum level and potentially a reduction in efficacy.
Venlafaxine Venlafaxine may increase the excretion rate of Copanlisib which could result in a lower serum level and potentially a reduction in efficacy.
Trazodone The metabolism of Copanlisib can be decreased when combined with Trazodone.
Dexamethasone acetate The metabolism of Copanlisib can be increased when combined with Dexamethasone acetate.
Mibefradil The serum concentration of Copanlisib can be increased when it is combined with Mibefradil.
Vandetanib Vandetanib may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Simeprevir The metabolism of Copanlisib can be decreased when combined with Simeprevir.
Palbociclib The metabolism of Copanlisib can be decreased when combined with Palbociclib.
Dacomitinib The metabolism of Copanlisib can be decreased when combined with Dacomitinib.
Glasdegib Glasdegib may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Fluconazole The metabolism of Copanlisib can be decreased when combined with Fluconazole.
Erythromycin The serum concentration of Copanlisib can be increased when it is combined with Erythromycin.
Reserpine The metabolism of Copanlisib can be increased when combined with Reserpine.
Sorafenib The metabolism of Copanlisib can be decreased when combined with Sorafenib.
Quinine The metabolism of Copanlisib can be increased when combined with Quinine.
Tamoxifen The metabolism of Copanlisib can be increased when combined with Tamoxifen.
Mifepristone The metabolism of Copanlisib can be increased when combined with Mifepristone.
Zonisamide The metabolism of Copanlisib can be decreased when combined with Zonisamide.
Lapatinib The metabolism of Copanlisib can be decreased when combined with Lapatinib.
Paliperidone The metabolism of Copanlisib can be decreased when combined with Paliperidone.
Elacridar Elacridar may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Brefeldin A The serum concentration of Copanlisib can be increased when it is combined with Brefeldin A.
Ivacaftor The serum concentration of Copanlisib can be increased when it is combined with Ivacaftor.
Linagliptin The metabolism of Copanlisib can be decreased when combined with Linagliptin.
Regorafenib Regorafenib may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Ponatinib The metabolism of Copanlisib can be decreased when combined with Ponatinib.
Afatinib Afatinib may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Ledipasvir Ledipasvir may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Vorapaxar The metabolism of Copanlisib can be decreased when combined with Vorapaxar.
Suvorexant The metabolism of Copanlisib can be decreased when combined with Suvorexant.
Netupitant The metabolism of Copanlisib can be decreased when combined with Netupitant.
Daclatasvir The metabolism of Copanlisib can be decreased when combined with Daclatasvir.
Rolapitant Rolapitant may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Venetoclax The metabolism of Copanlisib can be decreased when combined with Venetoclax.
Asunaprevir The metabolism of Copanlisib can be increased when combined with Asunaprevir.
Velpatasvir Velpatasvir may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Voxilaprevir Voxilaprevir may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Rucaparib The metabolism of Copanlisib can be decreased when combined with Rucaparib.
Enasidenib The metabolism of Copanlisib can be increased when combined with Enasidenib.
Pibrentasvir Pibrentasvir may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Glecaprevir The metabolism of Copanlisib can be decreased when combined with Glecaprevir.
Ivosidenib The metabolism of Copanlisib can be increased when combined with Ivosidenib.
Sildenafil The metabolism of Copanlisib can be decreased when combined with Sildenafil.
Simvastatin The metabolism of Copanlisib can be decreased when combined with Simvastatin.
Vardenafil The metabolism of Copanlisib can be decreased when combined with Vardenafil.
Dronedarone The metabolism of Copanlisib can be decreased when combined with Dronedarone.
Ticagrelor The metabolism of Copanlisib can be decreased when combined with Ticagrelor.
Lomitapide The metabolism of Copanlisib can be decreased when combined with Lomitapide.
Fedratinib The serum concentration of Copanlisib can be increased when it is combined with Fedratinib.
Istradefylline The metabolism of Copanlisib can be decreased when combined with Istradefylline.
Enzalutamide The metabolism of Copanlisib can be increased when combined with Enzalutamide.
Verapamil The metabolism of Copanlisib can be decreased when combined with Verapamil.
Norgestimate The metabolism of Copanlisib can be increased when combined with Norgestimate.
Methylene blue The serum concentration of Copanlisib can be increased when it is combined with Methylene blue.
Ripretinib Ripretinib may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Pralsetinib The metabolism of Copanlisib can be increased when combined with Pralsetinib.
Diosmin The serum concentration of Copanlisib can be increased when it is combined with Diosmin.
Levoketoconazole The metabolism of Copanlisib can be decreased when combined with Levoketoconazole.
Belumosudil Belumosudil may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Bexarotene The metabolism of Copanlisib can be increased when combined with Bexarotene.
Bosentan The metabolism of Copanlisib can be increased when combined with Bosentan.
Nafcillin The metabolism of Copanlisib can be increased when combined with Nafcillin.
Etravirine The metabolism of Copanlisib can be increased when combined with Etravirine.
Avasimibe The metabolism of Copanlisib can be increased when combined with Avasimibe.

Target Protein

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform PIK3CA
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform PIK3CD
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform PIK3CB
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform PIK3CG

Referensi & Sumber

Artikel (PubMed)
  • PMID: 29127587
    Markham A: Copanlisib: First Global Approval. Drugs. 2017 Dec;77(18):2057-2062. doi: 10.1007/s40265-017-0838-6.
  • PMID: 30147333
    Mensah FA, Blaize JP, Bryan LJ: Spotlight on copanlisib and its potential in the treatment of relapsed/refractory follicular lymphoma: evidence to date. Onco Targets Ther. 2018 Aug 13;11:4817-4827. doi: 10.2147/OTT.S142264. eCollection 2018.
  • PMID: 28714036
    Gerisch M, Schwarz T, Lang D, Rohde G, Reif S, Genvresse I, Reschke S, van der Mey D, Granvil C: Pharmacokinetics of intravenous pan-class I phosphatidylinositol 3-kinase (PI3K) inhibitor (14)Ccopanlisib (BAY 80-6946) in a mass balance study in healthy male volunteers. Cancer Chemother Pharmacol. 2017 Sep;80(3):535-544. doi: 10.1007/s00280-017-3383-9. Epub 2017 Jul 11.

Contoh Produk & Brand

Produk: 1 • International brands: 0
Produk
  • Aliqopa
    Injection, powder, lyophilized, for solution • 15 mg/1mL • Intravenous • US • Approved

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