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| Clinical data | |
|---|---|
| Trade names | Treanda, others |
| Other names | SDX-105 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a608034 |
| License data | |
| Routes of administration | Intravenous infusion |
| ATC code | |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Bioavailability | NA (intravenous only) |
| Protein binding | 94–96% |
| Metabolism | Hydrolyzed to inactive metabolites. Two minor metabolites (M3 and M4) formed byCYP1A2 |
| Eliminationhalf-life | 40 min (bendamustine), 3 h (M3), 30 min (M4) |
| Excretion | ~50% urinary, ~25% fecal[3] |
| Identifiers | |
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| CAS Number | |
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| IUPHAR/BPS | |
| DrugBank |
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| ChemSpider |
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| UNII | |
| ChEMBL | |
| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.205.789 |
| Chemical and physical data | |
| Formula | C16H21Cl2N3O2 |
| Molar mass | 358.26 g·mol−1 |
| 3D model (JSmol) | |
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Bendamustine, sold under the brand nameTreanda among others, is achemotherapy medication used in the treatment ofchronic lymphocytic leukemia (CLL),multiple myeloma, andnon-Hodgkin's lymphoma.[4][5] It is given byinjection into a vein.[4]
Common side effects includelow blood cell counts,fever,nausea,diarrhea, loss of appetite,cough, andrash.[4] Other severe side effects includeallergic reactions and increased risk of infection.[4] Use inpregnancy is known to harm the baby.[4] Bendamustine is in thealkylating agents drug class.[4] It works by interfering with the function ofDNA andRNA.[4]
Bendamustine was approved for medical use in the United States in 2008.[4] It is on theWorld Health Organization's List of Essential Medicines.[6][7] It was originally made fromnitrogen mustard.[4]
One combination for stage III/IV relapsed or refractory indolentlymphomas andmantle cell lymphoma (MCL), with or without prior rituximab-containing chemoimmunotherapy treatment, is bendamustine with mitoxantrone and rituximab.[8] In Germany in 2012 it has become the first line treatment of choice for indolent lymphoma.[9] Trial results released in June 2012 showed that it more than doubled diseaseprogression-free survival when given along withrituximab. The combination also left patients with fewer side effects than the olderR-CHOP treatment.[10]
Common adverse reactions are typical for the class ofnitrogen mustards, and include nausea, fatigue, vomiting, diarrhea, fever, constipation, loss of appetite, cough, headache, unintentional weight loss, difficulty breathing, rashes, andstomatitis, as well as immunosuppression, anemia, andlow platelet counts. Notably, this drug has a low incidence of hair loss (alopecia) unlike most other chemotherapy drugs.[11]
Bendamustine is a white, water-soluble microcrystalline powder withamphoteric properties. It acts as analkylating agent causing intra-strand and inter-strand cross-links betweenDNA bases.
After intravenous infusion, it is extensively metabolised in theliver bycytochrome p450. More than 95% of the drug is bound to protein – primarilyalbumin. Only free bendamustine is active. Elimination is biphasic, with a half-life of 6–10 minutes and a terminal half-life of approximately 30 minutes. It is eliminated primarily through thekidneys.
Bendamustine was first made in 1963 by Ozegowski and Krebs inEast Germany (the former German Democratic Republic).[12] Until 1990 it was available only in East Germany. East German researchers found that it was useful for treatingchronic lymphocytic leukemia,Hodgkin's disease,non-Hodgkin's lymphoma,multiple myeloma andlung cancer.
Bendamustine received its first marketing approval in Germany, where it is marketed under the tradename Ribomustin, by Astellas Pharma GmbH's licensee, Mundipharma International Corporation Limited. It is indicated as a single-agent or in combination with other anti-cancer agents for indolentnon-Hodgkin's lymphoma, multiple myeloma, and chronic lymphocytic leukemia. SymBio Pharmaceuticals Ltd. holds exclusive rights to develop and market bendamustine HCl in Japan and selected Asia Pacific Rim countries.
In March 2008,Cephalon received approval from theUnited StatesFood and Drug Administration to market bendamustine in the US, where it is sold under the tradename Treanda, for treatment of chronic lymphocytic leukemia.[13]
In October 2008, the FDA granted further approval to market Treanda for the treatment of indolent B-cell non-Hodgkin's lymphoma that has progressed during or within six months of treatment with rituximab or a rituximab-containing regimen.[14]
It is also being studied for the treatment ofsarcoma.[15] It is also being investigated in phase II trials for the non-cancer treatment ofAL amyloidosis.[16]
