Peringatan Keamanan

The lowest lethal dose (LDLo) in rats is >2000 mg/kg following oral administration and >40 mg/kg following intravenous administration.L31613 The oral Lowest published toxic dose (TDLo) in humans is 9 mg/kg/4W (intermittent).L31623

There is limited clinical experience in managing lenalidomide overdose. In single-dose studies, healthy subjects have been exposed to doses up to 400 mg. In clinical trials, the dose-limiting toxicity was neutropenia and thrombocytopenia. Toxicities associated with lenalidomide, some leading to fatality, include embryo-fetal toxicity, neutropenia, thrombocytopenia, venous (deep vein thrombosis and pulmonary embolism) and arterial thromboembolic events (myocardial infarction and stroke), serious adverse cardiovascular reactions, second primary malignancies, hepatotoxicity, severe cutaneous reactions, tumour lysis syndrome, tumour flare reaction, hypothyroidism, and hyperthyroidism.L16028

Lenalidomide

DB00480

small molecule approved

Deskripsi

Lenalidomide (previously referred to as CC-5013) is an immunomodulatory drug with potent antineoplastic, anti-angiogenic, and anti-inflammatory properties.A228553 It is a 4-amino-glutamyl analogue of thalidomide A228543 and like thalidomide, lenalidomide exists as a racemic mixture of the active S(-) and R(+) forms.A228708 However, lenalidomide is much safer and potent than thalidomide, with fewer adverse effects and toxicities.A714, A228543 Thalidomide and its analogues, including lenalidomide, are referred to as immunomodulatory imide drugs (also known as cereblon modulators), which are a class of immunomodulatory drugs that contain an imide group. Lenalidomide works through various mechanisms of actions that promote malignant cell death and enhance host immunity.A228708 Available as oral capsules, lenalidomide is approved by the FDA and EU for the treatment of multiple myeloma, myelodysplastic syndromes, mantle cell lymphoma, follicular lymphoma, and marginal zone lymphoma in selected patients.L16028 Due to severe teratogenicity, pregnancy must be excluded before the start of treatment and patients must enroll in the lenalidomide Risk Evaluation and Mitigation Strategy (REMS) program to ensure contraception adherence.A228708

Struktur Molekul 2D

Berat 259.2606
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) In healthy subjects, the mean half-life of lenalidomide is three hours in the clinically relevant dose range (5–50 mg).[A228628] Half-life can range from three to five hours in patients with multiple myeloma, myelodysplastic syndromes, or mantle cell lymphoma.[L16028]
Volume Distribusi In healthy male subjects, the apparent volume of distribution was 75.8 ± 7.3 L.[A228628]
Klirens (Clearance) The renal clearance of lenalidomide exceeds the glomerular filtration rate.[L16028] In healthy male subjects, the oral clearance was 318 ± 41 mL/min.[A228628]

Absorpsi

Following oral administration, lenalidomide is rapidly absorbed with high bioavailability.A228628 It has a Tmax ranging from 0.5 to six hours. Lenalidomide exhibits a linear pharmacokinetic profile, with its AUC and Cmax increasing proportionally with dose. Multiple dosing does not result in drug accumulation.L16028 In healthy male subjects, the Cmax was 413 ± 77 ng/ml and the AUCinfinity was 1319 ± 162 h x ng/ml.A228628

Metabolisme

Lenalidomide is not subject to extensive hepatic metabolism involving CYP enzymes and metabolism contributes to a very minor extent to the clearance of lenalidomide in humans. Lenalidomide undergoes hydrolysis in human plasma to form 5-hydroxy-lenalidomide and N-acetyl-lenalidomide.A228628 Unchanged lenalidomide is the predominant circulating drug form, with metabolites accounting for less than five percent of the parent drug levels in the circulation.L16028

Rute Eliminasi

Lenalidomide is eliminated predominantly via urinary excretion in the unchanged form. Following oral administration of 25 mg of radiolabeled lenalidomide in healthy subjects, about 90% of the dose (4.59% as metabolites) was eliminated in urine and 4% of the dose (1.83% as metabolites) was eliminated in feces within ten days post-dose. Approximately 85% of the dose was excreted as lenalidomide in the urine within 24 hours.L16028

Interaksi Makanan

2 Data
  • 1. Take at the same time every day. Skip the missed dose if it has been more than 12 hours since your regular time.
  • 2. Take with or without food. High-fat meals decrease absorption, but not to a clinically significant extent.

Interaksi Obat

1196 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Lenalidomide.
Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Lenalidomide.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Lenalidomide.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Lenalidomide.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Lenalidomide.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Lenalidomide.
Anakinra The risk or severity of adverse effects can be increased when Anakinra is combined with Lenalidomide.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Lenalidomide.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Lenalidomide.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Lenalidomide.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Lenalidomide.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Lenalidomide.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Lenalidomide.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Lenalidomide.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Lenalidomide.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Lenalidomide.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Lenalidomide.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Lenalidomide.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Lenalidomide.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Lenalidomide.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Lenalidomide.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Lenalidomide.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Lenalidomide.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Lenalidomide.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Lenalidomide.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Lenalidomide.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Lenalidomide.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Lenalidomide.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Lenalidomide.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Lenalidomide.
Cladribine Lenalidomide may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Lenalidomide.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Lenalidomide.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Lenalidomide.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Lenalidomide.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Lenalidomide.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Lenalidomide.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Lenalidomide.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Lenalidomide.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Lenalidomide.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Lenalidomide.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Lenalidomide.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Lenalidomide.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Lenalidomide.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Lenalidomide.
Sorafenib The risk or severity of adverse effects can be increased when Sorafenib is combined with Lenalidomide.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Lenalidomide.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Lenalidomide.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Lenalidomide.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Lenalidomide.
Teniposide The risk or severity of adverse effects can be increased when Teniposide is combined with Lenalidomide.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Lenalidomide.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Lenalidomide.
Altretamine The risk or severity of adverse effects can be increased when Lenalidomide is combined with Altretamine.
Zidovudine The risk or severity of adverse effects can be increased when Lenalidomide is combined with Zidovudine.
Cisplatin The risk or severity of adverse effects can be increased when Lenalidomide is combined with Cisplatin.
Oxaliplatin The risk or severity of adverse effects can be increased when Lenalidomide is combined with Oxaliplatin.
Cyclophosphamide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Cyclophosphamide.
Vincristine The risk or severity of adverse effects can be increased when Lenalidomide is combined with Vincristine.
Fluorouracil The risk or severity of adverse effects can be increased when Lenalidomide is combined with Fluorouracil.
Propylthiouracil The risk or severity of adverse effects can be increased when Lenalidomide is combined with Propylthiouracil.
Pentostatin The risk or severity of adverse effects can be increased when Lenalidomide is combined with Pentostatin.
Methotrexate The risk or severity of adverse effects can be increased when Lenalidomide is combined with Methotrexate.
Carbamazepine The risk or severity of adverse effects can be increased when Lenalidomide is combined with Carbamazepine.
Vinblastine The risk or severity of adverse effects can be increased when Lenalidomide is combined with Vinblastine.
Fluticasone propionate The risk or severity of adverse effects can be increased when Lenalidomide is combined with Fluticasone propionate.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Fluocinolone acetonide.
Linezolid The risk or severity of adverse effects can be increased when Lenalidomide is combined with Linezolid.
Imatinib The risk or severity of adverse effects can be increased when Lenalidomide is combined with Imatinib.
Triamcinolone The risk or severity of adverse effects can be increased when Lenalidomide is combined with Triamcinolone.
Clofarabine The risk or severity of adverse effects can be increased when Lenalidomide is combined with Clofarabine.
Prednisone The risk or severity of adverse effects can be increased when Lenalidomide is combined with Prednisone.
Pemetrexed The risk or severity of adverse effects can be increased when Lenalidomide is combined with Pemetrexed.
Fludrocortisone The risk or severity of adverse effects can be increased when Lenalidomide is combined with Fludrocortisone.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Lenalidomide is combined with Mycophenolate mofetil.
Daunorubicin The risk or severity of adverse effects can be increased when Lenalidomide is combined with Daunorubicin.
Irinotecan The risk or severity of adverse effects can be increased when Lenalidomide is combined with Irinotecan.
Methimazole The risk or severity of adverse effects can be increased when Lenalidomide is combined with Methimazole.
Etoposide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Etoposide.
Sulfasalazine The risk or severity of adverse effects can be increased when Lenalidomide is combined with Sulfasalazine.
Dacarbazine The risk or severity of adverse effects can be increased when Lenalidomide is combined with Dacarbazine.
Temozolomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Temozolomide.
Penicillamine The risk or severity of adverse effects can be increased when Lenalidomide is combined with Penicillamine.
Prednisolone The risk or severity of adverse effects can be increased when Lenalidomide is combined with Prednisolone.
Sirolimus The risk or severity of adverse effects can be increased when Lenalidomide is combined with Sirolimus.
Mechlorethamine The risk or severity of adverse effects can be increased when Lenalidomide is combined with Mechlorethamine.
Azacitidine The risk or severity of adverse effects can be increased when Lenalidomide is combined with Azacitidine.
Carboplatin The risk or severity of adverse effects can be increased when Lenalidomide is combined with Carboplatin.
Methylprednisolone The risk or severity of adverse effects can be increased when Lenalidomide is combined with Methylprednisolone.
Dactinomycin The risk or severity of adverse effects can be increased when Lenalidomide is combined with Dactinomycin.
Cytarabine The risk or severity of adverse effects can be increased when Lenalidomide is combined with Cytarabine.
Azathioprine The risk or severity of adverse effects can be increased when Lenalidomide is combined with Azathioprine.
Doxorubicin The risk or severity of adverse effects can be increased when Lenalidomide is combined with Doxorubicin.
Hydroxyurea The risk or severity of adverse effects can be increased when Lenalidomide is combined with Hydroxyurea.
Busulfan The risk or severity of adverse effects can be increased when Lenalidomide is combined with Busulfan.
Mycophenolic acid The risk or severity of adverse effects can be increased when Lenalidomide is combined with Mycophenolic acid.
Topotecan The risk or severity of adverse effects can be increased when Lenalidomide is combined with Topotecan.
Mercaptopurine The risk or severity of adverse effects can be increased when Lenalidomide is combined with Mercaptopurine.
Thalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Lenalidomide is combined with Melphalan.

Target Protein

Tumor necrosis factor TNF
Protein cereblon CRBN
Tumor necrosis factor ligand superfamily member 11 TNFSF11
Cadherin-5 CDH5
Prostaglandin G/H synthase 2 PTGS2

Referensi & Sumber

Synthesis reference: Surya Narayana Devarakonda, Sesha Reddy Yarraguntla, Vamsi Krishna Mudapaka, Rajasekhar Kadaboina, Veerender Murki, Amarendhar Manda, Venkata Rao Badisa, Naresh Vemula, Rama Seshagiri Rao Pulla, Venu Nalivela, "PREPARATION OF LENALIDOMIDE." U.S. Patent US20110021567, issued January 27, 2011.
Artikel (PubMed)
  • PMID: 16569772
    Chang DH, Liu N, Klimek V, Hassoun H, Mazumder A, Nimer SD, Jagannath S, Dhodapkar MV: Enhancement of ligand-dependent activation of human natural killer T cells by lenalidomide: therapeutic implications. Blood. 2006 Jul 15;108(2):618-21. Epub 2006 Mar 28.
  • PMID: 16344099
    Anderson KC: Lenalidomide and thalidomide: mechanisms of action--similarities and differences. Semin Hematol. 2005 Oct;42(4 Suppl 4):S3-8.
  • PMID: 19674465
    Kotla V, Goel S, Nischal S, Heuck C, Vivek K, Das B, Verma A: Mechanism of action of lenalidomide in hematological malignancies. J Hematol Oncol. 2009 Aug 12;2:36. doi: 10.1186/1756-8722-2-36.
  • PMID: 25947406
    Qiao SK, Guo XN, Ren JH, Ren HY: Efficacy and Safety of Lenalidomide in the Treatment of Multiple Myeloma: A Systematic Review and Meta-analysis of Randomized Controlled Trials. Chin Med J (Engl). 2015 May 5;128(9):1215-22. doi: 10.4103/0366-6999.156134.
  • PMID: 22037879
    Chen N, Wen L, Lau H, Surapaneni S, Kumar G: Pharmacokinetics, metabolism and excretion of (14)C-lenalidomide following oral administration in healthy male subjects. Cancer Chemother Pharmacol. 2012 Mar;69(3):789-97. doi: 10.1007/s00280-011-1760-3. Epub 2011 Oct 29.
  • PMID: 26438514
    Fink EC, Ebert BL: The novel mechanism of lenalidomide activity. Blood. 2015 Nov 19;126(21):2366-9. doi: 10.1182/blood-2015-07-567958. Epub 2015 Oct 5.
  • PMID: 19236186
    Galustian C, Dalgleish A: Lenalidomide: a novel anticancer drug with multiple modalities. Expert Opin Pharmacother. 2009 Jan;10(1):125-33. doi: 10.1517/14656560802627903.
  • PMID: 16510725
    Kiaei M, Petri S, Kipiani K, Gardian G, Choi DK, Chen J, Calingasan NY, Schafer P, Muller GW, Stewart C, Hensley K, Beal MF: Thalidomide and lenalidomide extend survival in a transgenic mouse model of amyotrophic lateral sclerosis. J Neurosci. 2006 Mar 1;26(9):2467-73. doi: 10.1523/JNEUROSCI.5253-05.2006.

Contoh Produk & Brand

Produk: 236 • International brands: 2
Produk
  • Apo-lenalidomide
    Capsule • 2.5 mg • Oral • Canada • Generic • Approved
  • Apo-lenalidomide
    Capsule • 5 mg • Oral • Canada • Generic • Approved
  • Apo-lenalidomide
    Capsule • 10 mg • Oral • Canada • Generic • Approved
  • Apo-lenalidomide
    Capsule • 15 mg • Oral • Canada • Generic • Approved
  • Apo-lenalidomide
    Capsule • 20 mg • Oral • Canada • Generic • Approved
  • Apo-lenalidomide
    Capsule • 25 mg • Oral • Canada • Generic • Approved
  • Eugia-lenalidomide
    Capsule • 2.5 mg • Oral • Canada • Approved
  • Eugia-lenalidomide
    Capsule • 5 mg • Oral • Canada • Approved
Menampilkan 8 dari 236 produk.
International Brands
  • Ladevina
  • Lenangio

Sekuens Gen/Protein (FASTA)

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