Chloroambucil - CAS 305-03-3
Catalog number: 305-03-3
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C14H19Cl2NO2
Molecular Weight:
304.21
COA:
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Targets:
Others
Description:
Chlorambucil (marketed as Leukeran by GlaxoSmithKline) is a chemotherapy drug that has been mainly used in the treatment of chronic lymphocytic leukemia. It is a nitrogen mustard alkylating agent and can be given orally. It is on the World Health Organization's List of Essential Medicines, a list of the most important medication needed in a basic health system.
Purity:
>98%
Synonyms:
Chlorambucil
MSDS:
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InChIKey:
JCKYGMPEJWAADB-UHFFFAOYSA-N
InChI:
InChI=1S/C14H19Cl2NO2/c15-8-10-17(11-9-16)13-6-4-12(5-7-13)2-1-3-14(18)19/h4-7H,1-3,8-11H2,(H,18,19)
Canonical SMILES:
C1=CC(=CC=C1CCCC(=O)O)N(CCCl)CCCl
1.Evolving Strategies for the Treatment of Chronic Lymphocytic Leukemia in the Upfront Setting.
Bachow SH1, Lamanna N2,3. Curr Hematol Malig Rep. 2016 Feb;11(1):61-70. doi: 10.1007/s11899-016-0298-1.
Chronic lymphocytic leukemia (CLL) is a disease of marked clinical heterogeneity, and while some patients have a normal life expectancy, others develop rapidly progressive disease shortly after diagnosis. The current standard for upfront treatment of CLL is chemoimmunotherapy for younger fit patients, FCR (fludarabine, cyclophosphamide, and rituximab) being the prototype. For older patients, BR (bendamustine and rituximab) exhibits excellent activity with decreased toxicity. For the frailest patients, CD20 monoclonal antibodies with or without chlorambucil have proven to be efficacious. The novel oral kinase inhibitors ibrutinib and idelalisib are FDA-approved in the relapsed/refractory setting, and ibrutinib is approved upfront for those with del(17p). These drugs have produced long-term durable responses in the relapsed/refractory setting, and studies are underway using these as single agent upfront or in combination with both chemotherapy and monoclonal antibodies.
2.Managing Infusion-Related Reactions for Patients With Chronic Lymphocytic Leukemia Receiving Obinutuzumab.
Dawson K1, Moran M2, Guindon K1, Wan H3. Clin J Oncol Nurs. 2016 Apr 1;20(2):E41-8. doi: 10.1188/16.CJON.E41-E48.
BACKGROUND: In patients with previously untreated chronic lymphocytic leukemia (CLL) and comorbidities, treatment with the glycoengineered, type II anti-CD20 monoclonal antibody obinutuzumab (Gazyva®) (GA101) plus chlorambucil (Leukeran®) was associated with superior outcomes to rituximab (Rituxan®) plus chlorambucil, with a similar safety profile. However, a higher occurrence of infusion-related reactions (IRRs) was reported with obinutuzumab. These reactions typically require additional management.
3.Cost-Effectiveness of First-Line Chronic Lymphocytic Leukemia Treatments When Full-Dose Fludarabine Is Unsuitable.
Soini E1, Hautala A2, Poikonen E3, Becker U4, Kyttälä M2, Martikainen J5. Clin Ther. 2016 Mar 9. pii: S0149-2918(16)30056-X. doi: 10.1016/j.clinthera.2016.02.005. [Epub ahead of print]
PURPOSE: The cost-effectiveness of first-line chronic lymphocytic leukemia treatments was assessed among patients unsuitable for full doses of fludarabine.
4.Chlorambucil for the treatment of patients with chronic lymphocytic leukemia (CLL) - a systematic review and meta-analysis of randomized trials.
Vidal L1,2, Gurion R1,2, Ram R1,3, Raanani P1,2, Bairey O1,2, Robak T4, Gafter-Gvili A1,5, Shpilberg O1,6. Leuk Lymphoma. 2016 Mar 16:1-11. [Epub ahead of print]
Randomized clinical trials that compared chlorambucil to different regimens, for patients with chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL) do not support an overall survival (OS) benefit. To assess the efficacy and safety of chlorambucil as frontline treatment, we conducted a systematic review and meta-analysis of randomized controlled trials. OS was the primary outcome. Meta-analysis of 18 trials that compared purine analogs, alkylators, alemtuzumab and ibrutinib to chlorambucil demonstrated no OS benefit for therapy without chlorambucil over chlorambucil (pooled HR 0.99, 95% CI 0.91-1.08; 4133 patients). PFS was longer with purine analogs compared with chlorambucil with an increased risk of infection. The risk of secondary malignancies was not increased with chlorambucil. In conclusion, our study showed that chlorambucil is an acceptable chemotherapy backbone for unfit patients with CLL. Purine analogs should be preferred in fit younger patients because of longer PFS.
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CAS 305-03-3 Chloroambucil

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