Peringatan Keamanan

Overdosage, including fatal overdosage, has been reported in patients taking ixazomib. Manifestations of overdosage include adverse reactions reported at the recommended dosage, including severe nausea, vomiting, diarrhea, aspiration pneumonia, multiple organ failure and death. There is no known specific antidote for ixazomib overdose and ixazomib is not dialyzable. In the event of an overdose, monitor the patient closely for adverse reactions and provide appropriate supportive care.L51234, L51239

Ixazomib

DB09570

small molecule approved investigational

Deskripsi

Ixazomib is a reversible proteasome inhibitor. Because it is a modified peptide boronic acid with one chiral center,A264329 it is considered a boronate proteasome inhibitor.A7948 More than 99% of the drug compound is the R-enantiomer.A264329

Ixazomib was approved by the FDA on November 20, 2015, making it the first oral proteasome inhibitor approved in the US.A264319 It was later approved by Health Canada on August 3, 2016,L51239 and by the EMA on November 21, 2016.L51244 It was also investigated in other hematological malignancies as well as other conditions, such as systemic light chain (AL) amyloidosis, graft-versus-host disease, and lupus nephritis.A264324

Struktur Molekul 2D

Berat 361.03
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal half-life (t1/2) of ixazomib was 9.5 days based on a population PK analysis.[L51234]
Volume Distribusi The steady-state volume of distribution is 543 L.[L51234]
Klirens (Clearance) Based on a population PK analysis, systemic clearance was approximately 1.9 L/hr with inter-individual variability of 44%.[L51234]

Absorpsi

Upon oral administration, ixazomib is rapidly absorbed A264329 with a Tmax of one hour.L51234 Based on population pharmacokinetic (PK) analysis, the mean absolute oral bioavailability was 58%. Ixazomib area under the curve (AUC) increases in a dose-proportional manner over a dose range of 0.2 to 10.6 mg. A food effect study conducted in patients with a single 4 mg dose of ixazomib showed that a high-fat meal decreased ixazomib AUC by 28% and Cmax by 69%.L51234

Metabolisme

After the oral administration of a radiolabeled dose, ixazomib represented 70% of total drug-related material in plasma.L51234 Ixazomib undergoes both CYP- and non-CYP-mediated metabolism, which is reported to be the major drug clearance mechanism.A264329 The major biotransformation pathways include hydrolysis, deboronation, and N-dealkylation, with drug metabolites not expected to retain pharmacological activity.A264329 At clinically relevant ixazomib concentrations, in vitro studies using human cDNA-expressed cytochrome P450 isozymes showed that no specific CYP isozyme predominantly contributes to ixazomib metabolism. At higher than clinical concentrations, ixazomib was metabolized by multiple CYP isoforms with estimated relative contributions of 3A4 (42%), 1A2 (26%), 2B6 (16%), 2C8 (6%), 2D6 (5%), 2C19 (5%) and 2C9 (< 1%).L51234

Rute Eliminasi

After administration of a single oral dose of 14C-ixazomib to 5 patients with advanced cancer, 62% of the administered radioactivity was excreted in urine and 22% in the feces. Unchanged ixazomib accounted for < 3.5% of the administered dose recovered in urine.L51234 Following weekly oral dosing, the accumulation ratio was determined to be two-fold.L51234

Interaksi Makanan

2 Data
  • 1. Avoid St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce the serum concentration of ixazomib.
  • 2. Take on an empty stomach. Food increases the absorption of ixazomib, take ixazomib dose at least one hour before and at least two hours after food.

Interaksi Obat

1122 Data
Modafinil The metabolism of Ixazomib can be increased when combined with Modafinil.
Armodafinil The metabolism of Ixazomib can be increased when combined with Armodafinil.
Metreleptin The metabolism of Ixazomib can be increased when combined with Metreleptin.
Crizotinib The metabolism of Ixazomib can be decreased when combined with Crizotinib.
Pitolisant The serum concentration of Ixazomib can be decreased when it is combined with Pitolisant.
Icosapent Icosapent may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Methotrexate Methotrexate may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Meloxicam The risk or severity of methemoglobinemia can be increased when Ixazomib is combined with Meloxicam.
Carprofen Carprofen may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Ibuprofen Ibuprofen may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefoperazone Cefoperazone may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefotetan Cefotetan may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefoxitin Cefoxitin may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Ceftizoxime Ceftizoxime may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Magnesium salicylate Magnesium salicylate may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Salsalate Salsalate may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Choline magnesium trisalicylate Choline magnesium trisalicylate may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefepime Cefepime may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefacetrile Cefacetrile may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Ceftibuten Ceftibuten may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cefpodoxime Cefpodoxime may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Antrafenine Antrafenine may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Aminophenazone Aminophenazone may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Antipyrine Antipyrine may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Tiaprofenic acid Tiaprofenic acid may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Hydrolyzed Cephalothin Hydrolyzed Cephalothin may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cephalothin Group Cephalothin Group may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Oxyphenbutazone Oxyphenbutazone may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Latamoxef Latamoxef may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Nimesulide Nimesulide may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Benoxaprofen Benoxaprofen may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Zomepirac Zomepirac may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Ceftobiprole Ceftobiprole may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Cimicoxib Cimicoxib may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Ceftaroline fosamil Ceftaroline fosamil may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Lornoxicam Lornoxicam may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Aceclofenac Aceclofenac may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Zaltoprofen Zaltoprofen may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Azapropazone Azapropazone may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Parecoxib Parecoxib may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Salicylamide Salicylamide may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Kebuzone Kebuzone may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Isoxicam Isoxicam may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Indoprofen Indoprofen may decrease the excretion rate of Ixazomib which could result in a higher serum level.
Ibuproxam Ibuproxam may decrease the excretion rate of Ixazomib which could result in a higher serum level.

Target Protein

Proteasome subunit beta type-5 PSMB5

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25302026
    Offidani M, Corvatta L, Caraffa P, Gentili S, Maracci L, Leoni P: An evidence-based review of ixazomib citrate and its potential in the treatment of newly diagnosed multiple myeloma. Onco Targets Ther. 2014 Sep 29;7:1793-800. doi: 10.2147/OTT.S49187. eCollection 2014.
  • PMID: 27668055
    Raedler LA: Ninlaro (Ixazomib): First Oral Proteasome Inhibitor Approved for the Treatment of Patients with Relapsed or Refractory Multiple Myeloma. Am Health Drug Benefits. 2016 Mar;9(Spec Feature):102-5.
  • PMID: 26846321
    Shirley M: Ixazomib: First Global Approval. Drugs. 2016 Mar;76(3):405-11. doi: 10.1007/s40265-016-0548-5.
  • PMID: 30117017
    Gupta N, Hanley MJ, Xia C, Labotka R, Harvey RD, Venkatakrishnan K: Clinical Pharmacology of Ixazomib: The First Oral Proteasome Inhibitor. Clin Pharmacokinet. 2019 Apr;58(4):431-449. doi: 10.1007/s40262-018-0702-1.

Contoh Produk & Brand

Produk: 12 • International brands: 1
Produk
  • Ninlaro
    Capsule • 4 mg/1 • Oral • US • Approved
  • Ninlaro
    Capsule • 3 mg/1 • Oral • US • Approved
  • Ninlaro
    Capsule • 2.3 mg/1 • Oral • US • Approved
  • Ninlaro
    Capsule • 2.3 mg • Oral • Canada • Approved
  • Ninlaro
    Capsule • 3 mg • Oral • Canada • Approved
  • Ninlaro
    Capsule • 4 mg • Oral • Canada • Approved
  • Ninlaro
    Capsule • 4 mg/1 • Oral • US • Approved
  • Ninlaro
    Capsule • 3 mg/1 • Oral • US • Approved
Menampilkan 8 dari 12 produk.
International Brands
  • Ninlaro

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