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美卡舍明注射剂(Mecasermin,Rdnaigf-1)

2011-07-31 13:57:16  作者:新特药房  来源:中国新特药网天津分站  浏览次数:466  文字大小:【】【】【
简介: 【中文名称】 基因重组胰岛素生长因子-1 【产品英文名称】 Mecasermin 【功效主治】 美卡舍明主要用于长期治疗严重原发性IGF-1缺乏的患儿,或者生长激素(GH)基因缺失且体内出现GH中和抗体患 ...

【中文名称】 基因重组胰岛素生长因子-1
【产品英文名称】 Mecasermin
【功效主治】
美卡舍明主要用于长期治疗严重原发性IGF-1缺乏的患儿,或者生长激素(GH)基因缺失且体内出现GH中和抗体患儿的生长不足。美卡舍明不能用于治疗继发性IGF-1缺乏(如因GH缺乏、营养不良、甲状腺机能减退或长期应用激素抗炎治疗所致的IGF-1缺乏)。
【化学成分】
美卡舍明(Mecasermin)即重组人胰岛素样生长因子-1(rh-IGF-1),是一种由70个氨基酸组成的单链多肽,其氨基酸序列与胰岛素大约有50%的同源性。

【药理作用】
IGF-1是生长激素的重要调节物质,它还具有许多重要的生理机能,如促进骨骼、器官和其他组织的生长,抑制肝糖生成、胰岛素分泌,参与神经系统的维护和再生等。

【药物相互作用】
目前尚未开展与美卡舍明有关的药物相互作用研究。当美卡舍明与其他降糖药合用时,可能增强IGF-1诱发的低血糖作用。美卡舍明与重组人生长激素(rh-GH)合用时应小心慎重,因为两者都是用于治疗生长不足,且两者作用机制和反馈机制密切相关。美卡舍明与用于治疗注意力缺陷障碍(ADD)、注意障碍多动综合征(ADHD)和发作性睡病等疾病的神经兴奋剂(包括哌甲酯、右旋哌甲酯、苯丙胺、右旋苯丙胺和去氧麻黄碱等)合用时,也应提高警惕。

【不良反应】
与所有蛋白质药物一样,美卡舍明也可能在部分患者体内诱发产生相应抗体。一项临床试验发现,在给予美卡舍明治疗2年内,23名原发性IGF-1缺乏的患儿中有14名体内出现了抗IGF-1抗体。不过,这些抗体并未引发严重的临床后果(如变态反应或生长减退)。

【禁忌症】
【产品规格】
10mg
【用法用量】
美卡舍明为一种澄清的无菌注射剂,规格为4ml:40mg。美卡舍明应采取个体化给药方式,其推荐初始剂量为0.04~0.08mg/kg(40~80μg/kg),一天2次,皮下注射。若患者在给药1周后耐受良好,美卡舍明每次给药剂量可增大0.04mg/kg,直到最大剂量0.12mg/kg(1天2次)。研究者尚未在原发性IGF-1缺乏的患儿中评价过0.12mg/kg以上剂量的临床表现,而且由于可能发生低血糖反应,因此建议美卡舍明给药剂量不要超过0.12mg/kg。
   
如果患者在注射推荐剂量美卡舍明,同时摄取足够食物的情况下,仍然出现低血糖反应,则应适度减少美卡舍明给药剂量。美卡舍明应在进餐或进食前后短时间(约20分钟)内给药。若患者在给药前后无法进食,则应取消此次给药。而且在下次给药时,患者也不能因为前次取消给药而随意增加给药剂量。美卡舍明注射给药时应依次轮流更换不同的给药部位,不应固定在同一部位给药。

【贮藏方法】
美卡舍明应在2~8℃下避光保存,不可冷冻。当药瓶开启后,美卡舍明仍可在2~8℃下稳定保存30天。
【注意事项】
美卡舍明的使用应在医师指导下进行。美卡舍明尚未在2岁以下儿童中进行过研究。由于美卡舍明可像胰岛素一样引起低血糖反应,因此在美卡舍明给药前或给药后最好安排患者进餐或进食;年龄较小的患儿应特别注意,因为他们的进食时间常常不太固定。患者在注射美卡舍明后2~3小时内(特别是在美卡舍明治疗初期)最好避免从事任何具有危险性的活动(如驾驶汽车等)。

SHORT DESCRIPTION: Increlex is a brand name (U.S.) for injectable IGF-1 (Insulin-like Growth Factor 1), manufactured by Tercica Inc. Mecasermin, which is the given generic name for rhIGF-1, was approved by the U.S. Food and Drug Administration in August 2005 for the treatment of growth deficiency in children. It is specifically indicated for severe primary IGF-1 deficiency (Primary IGFD), which is characterized by a failure to produce normal levels of IGF-1 due to inefficiencies in the Growth Hormone IGF-1 axis. The recommended starting dose for Increlex is .04 to .08 mg/kg, which is given twice per day. If this is well tolerated for one week the dose may be increased by .04 mg/kg per injection, to a maximum of .12 mg/kg (twice daily). Doses greater than 0.12 mg/kg twice daily are not recommended clinically, due to potential hypoglycemic effects. For the same reason, an upper ceiling of safety/comfort will be reached with most bodybuilders (this is not "more = better" type of drug). This will likely be extended over the .12 mg/kg recommendation (despite the recommendations against by the manufacturer) with some adventurous athletes, as they learn to exploit the hypoglycemic effects of IGF-1, taking it with a high level of simple carbohydrates during the post-training window. Despite the temptation, one should never begin using this drug at a high dosage! Minor side effects are intra cranial hypertension, which occurred in three subjects. In two subjects the events resolved without ceasing the drug, while in a third a short break and resumption at a lower dose resolved the issue. Mild elevations in the serum AST and LDH were found in a significant number of patients, but they were not significant enough to discontinue therapy.

LONG DESCRIPTION: Increlex is a brand name (U.S.) for injectable IGF-1 (Insulin-like Growth Factor 1), manufactured by Tercica Inc. of Brisbane California. Tercica licenses this technology from Genentech, which was the first company to sell a synthetically manufactured Human Growth Hormone product in the United States (Protropin). Like Human Growth Hormone, IGF-1 is a delicate and complex hormone. It consists of 70 amino acids in a single chain, with three disulfide bridges and a molecular weight of 7649 Daltons. Tercica's rhIGF-1 is produced by recombinant DNA technology, where it is synthesized by E. coli bacteria that have been modified by the addition of the human IGF-1 gene. The resulting product is identical to the endogenous IGF-1 protein, with all 70 amino acids in the proper sequence (unlike early high products like Protropin, which use slight variants of the active hormone).

Mecasermin, which is the given generic name for rhIGF-1, was approved by the U.S. Food and Drug Administration in August 2005 for the treatment of growth deficiency in children. It is specifically indicated for severe primary IGF-1 deficiency (Primary IGFD), which is characterized by a failure to produce normal levels of IGF-1 due to inefficiencies in the Growth Hormone IGF-1 axis. Such patients typically have normal or even high levels of Growth Hormone, but their bodies do not respond to it with the normal production of IGF-1. It is also indicated for the treatment of certain patients who have developed antibodies to Growth Hormone. In either case, the patient is not properly responsive to Growth Hormone therapy, making IGF-1 a very promising alternative medication. Tercica was granted Orphan Drug status for the use of Mecasermin to treat Primary IGFD, which means they have a market protected from competition (generic Mecasermin products) for a period of seven years.

Insulin-like Growth Factor-1 is a primary mediator of Growth Hormone's actions in the human body. GH binds to Growth Hormone receptors in the liver and peripheral tissues, and stimulates the synthesis and secretion of IGF-1. IGF-1, in turn, is the hormone actually responsible for the positive effects GH therapy has on skeletal muscle mass, whole body cell/organ growth, bone density, and linear (statural) growth. IGF-1 is also responsible for the known effect of Growth Hormone therapy on carbohydrate metabolism, namely reducing hepatic glucose production and stimulating peripheral glucose utilization. A good deal of research is being given to IGF-1 drugs in the treatment of certain forms of diabetes, and in December 2003 the FDA even granted Insmed Orphan Drug status for the use of Mecasermin Rinfibate (a similar medication not yet on the market) for the treatment of extreme Insulin resistance. Overall, Increlex will offer many of the same therapeutic benefits that are known of Growth Hormone. For our purposes this, of course, includes the support of muscle growth in adulthood, though this is not yet an approved use of the drug. Perhaps at some point we will see it approved for some newly recognized adult IGF-1 deficiency, like rHGH was for adult GH deficiency. Until then, it will likely remain an expensive drug, marketed exclusively to a small population of patients.

Although IGF-1 is a primary mediator of the effects, it is important to point out that it is not the sole mediator of them. GH does have some inherent effects in the body. The most notably of these is an effect of body fat deposition. GH has a Strong lipolytic effect, which can be so direct and measurable that patients commonly notice a reduction of fat even around the site of injection. This trait is lacking in IGF-1. In fact, a common documented side effect of Increlex therapy is lipohypertrophy (fat gain) around the site of injection's IGF-1 drug like this will, therefore, offer muscle growth benefits like (or better than) rHGH, but will not offer the same strong benefits on fat loss and muscle definition. These agents are more appropriately used during bulking phases of training, whereas Growth Hormone preparations will, likely, remain the preferred drugs of the "Growth Hormone and Related" class for cutting cycles.

Increlex comes as an aqueous solution, with each milliliter containing l0 mg of IGF-1 protein. It is intended to be administered subcutaneously, usually under small pinches of skin on the abdominal or thigh areas (like rHGH is usually administered). Due to the very fast metabolism of free IGF-1, the drug has a very short half-life in the body. Tercica's dosing recommendations call for an individual optimal dose to be determined, which is always based on twice daily application. The recommended starting dose is .04 to .08 mg/kg, which is given twice per day. If this is well tolerated for one week the dose may be increased by .04 mg/kg per injection, to a maximum of .12 mg/kg (twice daily). Doses greater than 0.12 mg/kg twice daily are not recommended clinically, due to potential hypoglycemic effects. For the same reason, an upper ceiling of safety/comfort will be reached with most bodybuilders (this is not "more = better" type of drug). This will likely be extended over the .12 mg/kg recommendation (despite the recommendations against by the manufacturer) with some adventurous athletes, as they learn to exploit the hypoglycemic effects of IGF-1, taking it with a high level of simple carbohydrates during the post-training window. Despite the temptation, one should never begin using this drug at a high dosage! If hypoglycemia occurs, despite adequate food intake, it is also important that the dose be reduced, for the sake of safety. Increlex should always be administered shortly before or after (20 minutes) a meal or snack as well, and never when simple carbohydrates are out of reach.

Unlike Increlex, which can be used for extended periods (years) in clinical medicine, bodybuilders would use this drug for shorter durations of 6-16 weeks. This is to minimize the potential for side effects or unwanted organ growth. As for an assessment of its general safety, we can note that medical data seems very favorable when the drug is administered correctly. During clinical studies with 71 subjects with Primary IGFD treated for a mean duration of 3.9 years, Increlex was very well tolerated, and none of the subjects withdrew from clinical study due to side effects or safety concerns. The most common side effect was hypoglycemia, which was reported by 42% of subjects on at least one occasion during therapy. This drug does, indeed, have a strong Insulin-like effect, which should be monitored. Most cases of hypoglycemia were mild, although five subjects had severe hypoglycemia requiring medical treatment, four of which experienced hypoglycemic seizures or loss of consciousness on one or more occasion. Symptomatic hypoglycemia was generally avoided when a meal or snack was consumed shortly before or after the administration of the drug. Enlargement of the tonsils occurred in 15% of patients during the first 1 to 2 years of therapy with lesser growth was noted in later years. Seven subjects required tonsillectomy.

Other minor side effects included intra cranial hypertension, which occurred in three subjects. In two subjects the events resolved without ceasing the drug, while in a third a short break and resumption at a lower dose resolved the issue. Mild elevations in the serum AST and LDH were found in a significant number of patients, but they were not significant enough to discontinue therapy. ALT elevations were occasionally noted as well, but again were not serious. Renal hypertrophy was shown to be rapid during the early years of therapy, although renal function remained normal in all patients. Elevations in cholesterol and triglycerides were observed, but remained within the upper limit of normal values. Evidence of heart enlargement was observed in a few individuals without clinical symptoms. The overall relationship between drug use and cardiac changes, however, has not yet been fully assessed. Thickening of facial soft tissues was observed in several patients, and should be monitored during therapy. Overall, the drug seems well tolerated, with a side effect profile that is not that far out of line with what we know of Growth Hormone drugs.

IGF-1 is known to be a potent stimulator of human muscle growth. We have seen drugs of this class, namely Long R3 IGF-1, work very well on very many occasions in the past. In some instances, this has been to an extent that might be called remarkable by the user. We wouldn't go so far as to call for an abandonment of steroids, however, as we still believe steroids are far more reliable and effective for the average user. The gains with IGF-l, though, are nothing to sneeze at in most cases. But with Long-R3, we also must remember that we have a synthetic compound with as of yet unverified safety in humans. It is an "experimental drug", used on animals only. We know it works on humans, but we don't have much safety data behind it. Increlex, on the other hand, is an approved drug in the U,S., and has been the subject of a great amount of research before reaching such a state. Though not yet approved for adult use, we can feel fairly comfortable with this drug. IGF-1 is admittedly a powerful "whole body" anabolic agent, and carries potential risks relating to organ growth if abused. These should never be ignored. But for those who are looking for safe and sane experimentation with an IGF-1 class drug, and would prefer an FDA approved medication over experimental compounds, you need look no further (provided you can find a way to purchase it, that is).

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