快樂小藥師 Im pharmacist nichts glücklich

The US Food and Drug Administration (FDA) announced today the approval of once-daily rilpivirine (Edurant, Tibotec Therapeutics, a division of Centocor Ortho Biotech Inc) for treatment of HIV infection. Rilpivirine is a nonnucleoside reverse transcriptase inhibitor (NNRTI) that may be taken once daily in combination with other antiretroviral drugs for HIV-infected, treatment-naive patients.  

"Patients may respond differently to various HIV drugs or experience varied side effects. FDA's approval of Edurant provides an additional treatment option for patients who are starting HIV therapy," said Edward Cox, MD, MPH, director of the Office of Antimicrobial Products in the FDA's Center for Drug Evaluation and Research.

The new drug gives clinicians an alternative to efavirenz, which has been considered the "gold standard" NNRTI — no other NNRTI has matched its efficacy since its approval in 1998. However, last summer, 2 phase 3 clinical trials of 1368 patients comparing rilpivirine with efavirenz revealed similar success rates: 83% of patients taking rilpivirine and 80% of patients taking efavirenz had undetectable amounts viral loads after 48 weeks of treatment. Each study enrolled about 700 patients.

In the studies, rilpivirine was associated with fewer adverse effects (especially central nervous system effects) and less lipid elevation. However, patients taking rilpivirine were more likely to experience virologic failure. Furthermore, virologic failure with rilpivirine resulted in cross-resistance to etravirine, eliminating that drug from future regimens. Patients with higher viral load at start of treatment were more likely not to respond to rilpivirine.

Paul Sax, MD, clinical director, Division of Infectious Diseases and HIV Program at Brigham and Women's Hospital, Boston, Massachusetts, explains: "The results of the study demonstrated that [rilpivirine] was better tolerated than efavirenz overall, but somewhat less effective in patients who entered the study with viral loads more than 100,000; as a result, there is a trade-off in this high-viral-load population between tolerability and virologic efficacy."

Still, for many patients, the low adverse effect profile reduces a significant barrier to achieving optimal adherence to antiretroviral therapy, Jose Zuniga, PhD, MPH, president of the International Association of Physicians in AIDS Care, told Medscape Medical News. "The approval of the second-generation NNRTI rilpivirine is welcome news, specifically because of its potency and reduced side effect profile — both of which will help greater numbers of treatment-naive patients achieve and sustain viral suppression," he says.

According to Dr. Sax, a single-pill, once-daily coformulation of rilpivirine, tenofovir, and emtricitabine is currently in development.

美國食品和藥物管理局（FDA）20日宣佈，他們批准每日一次rilpivirine用於治療愛滋病毒感染。 Rilpivirine是一種非核苷逆轉錄酶抑制劑（NNRTI），每天同其他抗逆轉錄病毒藥物一起服用一次，可用於治療初期的愛滋病毒感染者。

“病人對不同的HIV藥物反應可能不同，所產生的藥物副作用也可能不同。FDA對Edurant的批准為那些剛剛接受治療的病人提供了一個額外的治療選擇”，Edward Cox醫師說，他是FDA藥物評估和研究中心抗菌產品辦公室的主任。
這種新藥為臨床醫生提供了新的選擇，因為以前他們只有efavirenz，這種藥一直被視為NNRTI的“黃金標準 - 自1998年批准以來沒有其他的NNRTI藥物能與它的療效相媲美。然而，就在去年夏天，1368位患者接受了efavirenz與rilpivirine第二期第三次的臨床試驗，結果顯示這兩種藥物的成功率類似：經過48周的治療之後，83％的服用rilpivirine的患者和80％的服用efavirenz患者身上檢測不到病毒負荷量。每種藥物的研究對象約700名病人。 
在研究中發現，服用rilpivirine的病人都伴隨少許副作用（尤其影響中樞神經系統），他們血脂升高較少。然而，患者服用rilpivirine後更可能出現病毒學失靈。此外，rilpivirine引起的病毒失靈會對etravirine產生交叉耐藥性，最終致使藥物失靈。病毒負荷量較高的患者開始治療時不大可能對rilpivirine回應。 

位於馬薩諸塞州波士頓的布萊罕和婦女醫院傳染病和愛滋病毒專案科的臨床主任，Paul Sax醫師解釋說：“研究結果表明，rilpivirine整體上的耐受性要比efavirenz好，但對於身體內病毒量超過10萬的病人有效性有點低。因此，這些身體內病毒量較高的群體在耐受性和病毒學效用之間有一個權衡。” 

不過，對許多病人來說，rilpivirine的低副作用為他們堅持這種最佳的抗逆轉錄病毒療法掃除了不小的障礙，Jose Zuniga醫師告訴《醫學資訊檢索》，他是國際愛滋病護理協會的主席。“第二代NNRTI rilpivirine得到批准的確是個好消息，尤其因為它藥效好，副作用少 - 這都將有助於更多的初治患者實現和維持病毒的控制”，他說。

Sax博士說， rilpivirine、tenofovi和emtricitabine的混合體藥片目前正在開發中。