Anger et al.公开了苯达莫司汀对浆细胞瘤病人成功应用的最初临床结果。苯达莫司汀从1971年到1992年以Cytostasan的商品名由耶拿制药公司生产。从1993年后，这种细胞生长抑制剂被ribosepharm GmbH公司以Ribomustine的商品名上市。
其剂量血癌为50～60 mg/m2/d,3～5天或每3～4周为100～120 mg/m2 ；实体瘤每4 周为120～150 mg/m2 ,每日1 次,30～60 min 静脉滴注。盐酸苯达莫司汀作为单用或联合化疗,对何杰金病和非何杰金淋巴瘤的治疗反应率分别为61%～97%和41%～48 %。
对多发性骨髓瘤病人,苯达莫司汀/泼尼松治疗的完全反应率较高(32 %) ,美法仑/ 泼尼松疗法反应更持久。在环磷酰胺、长春新碱、泼尼松治疗方案中,苯达莫司汀取代环磷酰胺,对发展中低度毒性非何杰金淋巴瘤有相似的反应率。在环磷酰胺、甲氨蝶呤、氟尿嘧啶治疗方案中,苯达莫司汀取代环磷酰胺,使转移性乳腺癌病人的缓解期从6.2 个月延长至15.2个月。
盐酸苯达莫司汀( bendamustine) 是双功能基烷化剂,体外对人卵巢癌和乳腺癌有细胞毒性,体外与环磷酰胺、美法仑(melphalan) 、卡莫司汀(carmustine)和顺铂有部分交叉耐受。对乳腺癌细胞系MCF7抑制细胞生长的IC50为138μmol/L,对顺铂抗药性卵巢癌细胞系A27802CP2 的IC50为157μmol/L ,对多柔比星抗药性乳腺癌细胞系MCF7AD 的IC50为187μmol/L。在等毒性浓度( IC50s)下,苯达莫司汀比美法仑、环磷酰胺或卡莫司汀引起更多的DNA 双螺旋断裂,比卡莫司汀或环磷酰胺作用更持久。
体外引起浓度依赖性的B2慢性淋巴细胞白血病(B2CLL) 细胞凋亡,与氟达拉滨(fludarabine) 合用,在48 h 内凋亡率高1.4 倍。在Ⅰ期临床试验中,苯达莫司汀60～80 mg/m2每周1次,至8周,对顽固性实体瘤病人引起持久性的全淋巴细胞减少,主要为B细胞毒性。4周后,外周血B细胞、自然杀伤细胞和T 细胞分别下降90%,70%和60%以上。
TreandaGeneric Name: bendamustine (BEN da MUS teen)Brand Names: Treanda——————————————————————-What is Treanda?Treanda (bendamustine) is a cancer medication that interferes with the growth of cancer cells and slows their growth and spread in the body.Treanda is used to treat chronic lymphocytic leukemia.It is also used to treat indolent B-cell non-Hodgkin lymphoma after other medications have been tried without successful treatment of thiscondition.Treanda may also be used for other purposes not listed here.——————————————————————-Important information about TreandaYou should not receive Treanda if you are allergic to bendamustine or mannitol (Osmitrol). Do not receive Treanda if you are pregnant.It could harm the unborn baby.Before you receive Treanda, tell your doctor if you have a weak immune system, fever or other signs of infection, a metabolic disorder or electrolyte imbalance, liver or kidney disease, or if you smoke.Tell your caregiver right away if you have a fever, chills, itching, or skin rash during or shortly after the Treanda injection.Other serious side effects to tell your doctor about include fever, chills, cough, sore throat, feeling short of breath, pale skin, easybruising or bleeding, unusual weakness, severe skin rash, weak pulse, muscle weakness, fast or slow heart rate, confusion, lower back pain, blood in your urine, urinating less than usual, or swelling, redness, or signs of where Treanda was injected.To be sure Treanda is not causing harmful effects, your blood may need to be tested often. Your kidney or liver function may also need to be tested. Visit your doctor regularly.——————————————————————-Before receiving TreandaYou should not receive Treanda if you are allergic to bendamustine or mannitol (Osmitrol).To make sure you can safely receive Treanda, tell your doctor if you have any of these other conditions:a weak immune system;fever or other signs of infection;a metabolic disorder or electrolyte imbalance;liver disease;kidney disease; orif you smoke.FDA pregnancy category D. Do not receive Treanda if you are pregnant.It could harm the unborn baby. Use effective birth control, and tell your doctor if you become pregnant during treatment.It is not known whether bendamustine passes into breast milk or if it could harm a nursing baby.Do not receive Treanda without telling your doctor if you are breast-feeding a baby.Some people receiving Treanda have developed certain types of cancers. It is not known whether this medication causes cancer.Talk with your doctor about the risks and benefits of using Treanda.——————————————————————-How is Treanda given?Treanda is injected into a vein through an IV. You will receive this injection in a clinic or hospital setting. Treanda must be given slowly, and the IV infusion can take at least 30 minutes to complete.Treanda is usually given for 2 days in a row every 21 to 28 days.You may receive up to 8 treatments total, depending on the condition being treated. Follow your doctor's instructions.You may be given other medications to help prevent certain side effects of Treanda.Tell your caregivers if you feel any burning, pain, or swelling around the IV needle when the medicine is injected.To be sure Treanda is not causing harmful effects, your blood may need to be tested often. Your kidney or liver function may also need to be tested. Visit your doctor regularly.——————————————————————-What happens if I miss a dose?Call your doctor for instructions if you miss an appointment for your Treanda injection.——————————————————————-What happens if I overdose?Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.Overdose symptoms may include drowsiness, tremors, slow or shallow breathing, loss of balance or coordination, or seizure (convulsions).——————————————————————-What should I avoid while receiving Treanda?Treanda may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.——————————————————————-Treanda side effectsSome people receiving a Treanda injection have had a reaction to the infusion (when the medicine is injected into the vein). Tell yourcaregiver right away if you have fever, chills, itching, or skin rash during or shortly after the injection. Get emergency medical help if you have any of these signs of an allergic reaction to Treanda: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Tell your caregivers at once if you have aserious side effect such as:fever, chills, body aches, flu symptoms, sores in your mouth and throat;pale skin, feeling light-headed or short of breath, rapid heart rate, trouble concentrating;easy bruising or bleeding, purple or red pinpoint spots under your skin, unusual weakness;cold symptoms such as stuffy nose, sneezing, cough, sore throat;lower back pain, blood in your urine, urinating less than usual or not at all;numbness or tingly feeling around your mouth;muscle weakness, tightness, or contraction, overactive reflexes;fast or slow heart rate, weak pulse, confusion;dry mouth, feeling very thirsty or hot, heavy sweating or hot and dry skin;severe blistering, peeling, and red skin rash; orpain, swelling, redness, skin changes, or signs of infection where the medicine was injected.Less serious Treanda side effects may include:mild nausea, vomiting, diarrhea, constipation, or upset stomach;swelling in your hands or feet;headache, dizziness, drowsiness;loss of appetite, weight loss; or mild skin rash.This is not a complete list of side effects and others may occur.Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.——————————————————————-What other drugs will affect Treanda?Tell your doctor about all other medications you use, especially:allopurinol (Zyloprim);carbamazepine (Carbatrol, Equetro, Tegretol);cimetidine (Tagamet);ciprofloxacin (Cipro);fluvoxamine (Luvox);omeprazole (Prilosec);thiabendazole (Mintezol); or a barbiturate such as butabarbital (Butisol), secobarbital(Seconal), phenobarbital (Solfoton), and others.This list is not complete and other drugs may interact with Treanda.Tell your doctor about all medications you use.This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.——————————————————————-Where can I get more information?Your doctor or pharmacist can provide more information about Treanda.Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect.Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy.Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment ofhealthcare practitioners.The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects.If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.
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