Lenalidomide hydrochloride - CAS 1243329-97-6
Catalog number: 1243329-97-6
Category: Inhibitor
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Lenalidomideis a derivative of thalidomide introduced in 2004. Lenalidomide (Revlimid, CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM.
Revlimid hydrochloride; CC-5013 hydrochloride; CC5013 hydrochloride; CC 5013 hydrochloride
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1.A phase I study of bendamustine, lenalidomide and rituximab in relapsed and refractory lymphomas.
Cheson BD1, Crawford J. Br J Haematol. 2015 May;169(4):528-33. doi: 10.1111/bjh.13321. Epub 2015 Mar 7.
Many patients with non-Hodgkin (NHL) or Hodgkin lymphoma (HL) relapse or are refractory to initial therapy and require additional options. Bendamustine (B), lenalidomide (L) and rituximab (R) each have activity in this setting. This study was performed to determine the safety of BLR and its optimal phase II dose. Patients with NHL or HL failing standard therapies received B (90 mg/m(2)  days 1, 2 every 28 days), and L (escalating from 5 mg 21/28 days) for six cycles, followed by 6 months of L. At the highest dose R 375 mg/m(2) on day one of each cycle was added for patients with B-NHL. Histologies included diffuse large B-cell lymphoma (DLBCL, 11), marginal zone lymphoma (3), HL (2), and one each of transformed follicular lymphoma, Sézary syndrome, Waldenström macroglobulinaemia and mantle cell lymphoma. Neutropenia was the most common grade 3 and 4 toxicity, but no maximum tolerated dose was identified. Of 20 patients, seven responded (35%), including four complete remissions, with five unmaintained responses from 28+ to 37+ months, including 2 DLBCL.
2.Ezatiostat hydrochloride for the treatment of myelodysplastic syndromes.
Mahadevan D1, Sutton GR. Expert Opin Investig Drugs. 2015 May;24(5):725-33. doi: 10.1517/13543784.2015.1021003. Epub 2015 Feb 27.
INTRODUCTION: Myelodysplastic syndromes (MDSs) are associated with significant morbidity due to ineffective hematopoiesis. Given the limited number of drugs approved by the FDA, there is a need for new therapeutic options. Ezatiostat is a novel agent targeting oxidative stress via inhibition of glutathione S-transferase 1.
3.Bendamustine in combination with thalidomide and dexamethasone is a viable salvage option in myeloma relapsed and/or refractory to bortezomib and lenalidomide.
Lau IJ1, Smith D, Aitchison R, Blesing N, Roberts P, Peniket A, Yong K, Rabin N, Ramasamy K. Ann Hematol. 2015 Apr;94(4):643-9. doi: 10.1007/s00277-014-2238-2. Epub 2014 Oct 28.
Treatment options are limited in myeloma relapsed or refractory to both bortezomib and lenalidomide (double-relapsed/refractory multiple myeloma; DRMM). Bendamustine is an antitumour agent that has efficacy in relapsed myeloma. We retrospectively analysed data from 30 DRMM patients who received a combination of bendamustine, thalidomide and dexamethasone (BTD) in 28-day treatment cycles. Bendamustine was administered with a cumulative dose of up to 200 mg/m(2). Thalidomide (50-150 mg) was given daily as tolerated, and dexamethasone was given at an equivalent dose of up to 160 mg per cycle. A median of 5 (2-9) treatment cycles were administered per patient. Twenty-six patients (87 %) achieved stable disease or better. At a median follow-up time of 12.1 (2.3-21.5) months, median (95 % CI) progression-free survival and overall survival were 4.0 (2.6-5.3) months and 7.2 (5.2-9.2) months, respectively. The most common grade 3-4 adverse events were haematological: anaemia (n = 8, 34.
4.A comprehensive review of lenalidomide therapy for B-cell non-Hodgkin lymphoma.
Witzig TE1, Nowakowski GS2, Habermann TM2, Goy A3, Hernandez-Ilizaliturri FJ4, Chiappella A5, Vitolo U5, Fowler N6, Czuczman MS4. Ann Oncol. 2015 Aug;26(8):1667-77. doi: 10.1093/annonc/mdv102. Epub 2015 Feb 23.
Lenalidomide is an oral non-chemotherapy immunomodulator with direct and indirect effects on non-Hodgkin lymphoma (NHL) cells and with single-agent activity in relapsed/refractory aggressive and indolent B-cell NHL, including mantle cell lymphoma (MCL), diffuse large B-cell lymphoma, and follicular lymphoma. Based on the pivotal phase II MCL-001 trial of lenalidomide in heavily pretreated patients with relapsed/refractory MCL, lenalidomide was approved by the US Food and Drug Administration for the treatment of relapsed/refractory MCL after failure of two prior therapies, one of which includes bortezomib, at a recommended starting dose of 25 mg on days 1-21 of each 28-day cycle. Lenalidomide enhanced the survival benefit in combination with rituximab in preclinical models, prompting clinical evaluation of the lenalidomide-rituximab (R2) combination. In phase II trials, lenalidomide 20 mg on days 1-21 in combination with different standard-dose rituximab schedules exhibited promising activity in both first-line and relapsed/refractory disease across multiple B-cell NHL subtypes.
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CAS 1243329-97-6 Lenalidomide hydrochloride

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