Lenalidomide - CAS 191732-72-6
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
PROTAC | TNF-alpha
Lenalidomide is an analog of thalidomide, a TNF-α production inhibitor. Lenalidomide can be utilized in PROTAC as an E3 ligase ligand for targeting cereblon, inducing ubiquitination and degradation of casein kinase (CK) 1α by E3 ubiquitin ligase. Lenalidomide has been developed for the treatment of multiple myeloma and myelodysplastic syndromes (MDS).
Off-white Solid
3-(4-Amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione; 3-(7-amino-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione
Shelf Life:
2 years
Melting Point:
>250ºC (dec.)
Canonical SMILES:
1.Oral Ixazomib, Lenalidomide, and Dexamethasone for Multiple Myeloma.
Moreau P, Masszi T, Grzasko N, Bahlis NJ, Hansson M, Pour L, Sandhu I, Ganly P, Baker BW, Jackson SR, Stoppa AM, Simpson DR, Gimsing P, Palumbo A, Garderet L, Cavo M, Kumar S, Touzeau C, Buadi FK, Laubach JP, Berg DT, Lin J, Di Bacco A, Hui AM, van de Vel N Engl J Med. 2016 Apr 28;374(17):1621-34. doi: 10.1056/NEJMoa1516282.
BACKGROUND: Ixazomib is an oral proteasome inhibitor that is currently being studied for the treatment of multiple myeloma.
2.A study of high-dose lenalidomide induction and low-dose lenalidomide maintenance therapy for patients with hypomethylating agent refractory myelodysplastic syndrome.
Cherian MA1, Tibes R2, Gao F3, Fletcher T1, Fiala M1, Uy GL1, Westervelt P1, Jacoby MA1, Cashen AF1, Stockerl-Goldstein K1, DiPersio JF1, Vij R1. Leuk Lymphoma. 2016 Apr 27:1-6. [Epub ahead of print]
Myelodysplastic syndromes (MDS) are clonal hematopoietic disorders characterized by bone marrow failure which frequently progress to acute myeloid leukemia. Patients who fail to respond to, or progress on first-line DNA hypomethylating agents (HMA) have a poor prognosis. Conventionally dosed lenalidomide has activity in 5q-MDS. In other subtypes, it may reduce RBC transfusion requirements but does not result in cytogenetic responses. We previously reported that high-dose lenalidomide induction (50 mg/day) results in complete remissions in a high fraction of patients. We, therefore, conducted a Phase 2 trial of the same regimen in MDS refractory to HMA. Marrow complete remissions were seen in 33% of patients and hematological improvement in 8% of patients. Significant infections complicated more than 50% of cases. Future trials to explore alternative dosing schedules of high-dose lenalidomide to increase efficacy while decreasing toxicity are warranted.
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CAS 191732-72-6 Lenalidomide

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