美国食品和药物管理局FDA批准Picato（巨大戟醇酯凝胶，0.015％，0.05％）用于光化性角化病（AK）的局部治疗。 AK是一种由累积日光暴露导致的癌前病变，有可能恶变为第二常见的皮肤癌—鳞状细胞癌（SCC）。 0.015%Picato凝胶用于治疗头面部AK，用法为每日1次，连用3天：0.05%Picato凝胶用于治疗躯干及四肢AK，用法为每日1次，连用2天。Picato凝胶是第一种也是唯一一种AK局部治疗药物，其使用时间可短至2或3天。 根据美国皮肤病学会（AAD），每5名美国人中有1名将在其一生中患皮肤癌。有研究表明，约65％的鳞状细胞癌源于未经治疗的光化性角化病，且AAD指南估计，60％的40岁以上易感者至少患有一处光化性角化病。 "因为没有办法预测哪些光化性角化病会恶化为皮肤癌，所以早期发现和治疗病变是关键，"纽约西奈山医疗中心皮肤科的巨大戟醇酯研究员Mark Lebwohl博士说。"这种新的治疗方法尤其令人激动的是，它的治疗疗程只有2或3天。" 在纳入了1000多名光化性角化病患者的4项3期临床研究中，与安慰剂（n=502）相比，有显著较高比例的接受Picato凝胶治疗的患者的用药区域的AK得到完全清除（n=503）。最常见的不良事件（AE）是局部皮肤反应（LSR），包括红疹、剥脱、结痂和肿胀。 PICATO® (ingenol mebutate)凝胶, 0.015% 为局部使用 PICATO®(ingenol mebutate)凝胶, 0.05%为局部使用 美国初次批准：2012年 适应证和用途 PICATO®凝胶是一种细胞死亡诱导剂适用于日光性角化症的局部治疗。 剂量和给药方法 （1）仅为局部使用；不是为口服，眼科，或阴道内使用。 （2）脸部和头皮上日光性角化症：应用PICATO®凝胶，0.015%至发病区每天1次共3连续天。 （3）躯干和四肢上日光性角化症：应用PICATO®凝胶，0.05%至发病区域每天1次共2连续天。 剂型和规格 含ingenol mebutate,0.015%或0.05%凝胶。 临床研究 1、脸部和头皮的日光性角化症 在两项双盲，赋形剂-对照，临床试验中547例脸部或头皮上有AK的成年受试者被随机化至治疗用或 PICATO®凝胶，0.015%或赋形剂凝胶连续3天，接着8周随访期。总共536例受试者(98%)完成这些研究。108例PICATO®凝胶-治疗受试者实现完全清除，在12个月时复发率为54%。 2、躯干和四肢日光性角化症 在两项双盲，赋形剂-对照临床试验中458例躯干或四肢上有AK成年受试者被随机化至治疗用或PICATO®凝胶，0.05%或赋形剂凝胶共2连续天。接着8周随访期。总共447例受试者(98%)完成这些研究。38例实现完全清除PICATO®凝胶-治疗受试者，在12个月时复发率为50%。 在四项III期临床研究超过1,000例日光性角化症患者，用Picato凝胶治疗(n=503)当与安慰剂(n=502)比较见到患者显著较高比例患者治疗区AKs完全清除。最常见不良事件(AEs)是局部皮肤反应(LSRs)，包括红斑，剥落/鳞状物，起痂和肿胀。 Picato gel (Ingenol Mebutate) •Picato gel is the first topical therapy to effectively treat actinic keratosis (AKs) in just two or three days. •Use in Australia has been approved by the Therapeutic Goods Administration (TGA) for the topical treatment of solar keratosis in adults. •It is available in two different dosage strengths depending on the specific areas of the body requiring treatment •Patients can expect up to 80-85% reduction in AKs following treatment •Picato gel is only available with a doctor’s prescription. Indications and Usage Picato® is indicated for the topical treatment of actinic keratosis. Important Safety Information For topical use only; not for oral, ophthalmic, or intravaginal use. Eye disorders, including severe eye pain, eyelid edema, eyelid ptosis, periorbital edema can occur after exposure. Patients should wash hands well after applying Picato® gel, and avoid transfer of the drug to the periocular area during and after application. If accidental exposure occurs, flush eyes with water and seek medical care. Severe skin reactions in the treated areas on the face/scalp and trunk/extremities, including erythema, flaking/scaling, crusting, swelling, vesiculation/pustulation, and erosion/ulceration can occur after application. Administration of Picato® gel is not recommended until the skin is healed from any previous drug or surgical treatment. The most common adverse reactions observed in clinical trials on the face and scalp (≥2%) are local skin reactions (94%), application site pain (15%), application site pruritus (8%), application site infection (3%), periorbital edema (3%), and headache (2%). The most common adverse reactions observed in clinical trials on the trunk and extremities (≥2%) are local skin reactions (92%), application site pruritus (8%), application site irritation (4%), nasopharyngitis (2%), and application site pain (2%). There are no adequate and well-controlled studies of Picato® gel in pregnant women. Picato® gel should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. The safety and effectiveness of Picato® gel for actinic keratosis in patients less than 18 years of age have not been established. Picato 0.015 % topical gel    Picato 0.05 % topical gel