按照美国皮肤病学会(AAD)，1/5 美国人在其一生过程将发生皮肤癌[4]研究约65%鳞状细胞癌开始为未治疗的日光性角化症 [5] ，和AAD的指导原则估计60%易感人大于40有至少一处日光性角化症[6]。
纽约州纽约Mount Sinai 医学中心皮肤科ingenol mebutate研究者Dr. Mark Lebwohl说：“因为没有方法预测那个日光性角化症将进展为皮肤癌，病变的早期检测和治疗是至关重要的”“使这个新解决方案，特别令人兴奋的是两或三天的疗程。”
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® (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。(1)
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)
（2）脸部和头皮上日光性角化症：应用PICATO®凝胶， 0.015%至影响区每天1次共3连续天。(2) •
（3）躯干和四肢上日光性角化症：应用PICATO®凝胶，0.05%至影响区域每天1次共2连续天。(2)
剂型和规格
含ingenol mebutate, 0.015%或0.05%凝胶。(3)
禁忌证
无。4)
警告和注意事项
暴露后可能发生眼疾病，包括严重眼痛，眼睑水肿，眼睑下垂，眶周水肿。避免接触眼周区。如发生意外暴露，用水和冲洗眼睛和求医。(5.1)
可能发生局部皮肤反应包括严重反应(如，囊泡形成/脓泡形成，糜烂/溃疡)。来自任何以前药物或外科治疗皮肤愈合前建议不给予PICATO®凝胶。(5.2)
不良反应
最常见不良反应(≥2 %)是局部皮肤反应, 用药部位疼痛，用药部位瘙痒，用药部位刺激，用药部位感染，眶周水肿，鼻咽炎和头痛。(6.1)
为报告怀疑不良反应，联系LEO Pharma Inc.电话1-877-494-4536或FDA 电话1-800-FDA-1088或www.fda.gov/medwatch.
一般描述
PICATO®(ingenol mebutate)凝胶，0.015%或0.05%是一种澄明无色凝胶为局部给药, 含活性物质ingenol mebutate，一种细胞死亡诱导剂。
Manufacturer:
LEO Pharma Inc.
Active Ingredient(s):
Ingenol mebutate 0.015%, 0.05%; topical gel.
Indication(s):
Topical treatment of actinic keratosis (AK).
Pharmacology:
The mechanism of action by which ingenol mebutate induces cell death in treating actinic keratosis lesions is unknown.
Clinical Trials:
In two double-blind, vehicle-controlled, clinical trials (Study 1 and Study 2), 547 adult subjects with AK on the face or scalp were randomized to treatment with either Picato gel, 0.015% or vehicle gel for 3 consecutive days, followed by an 8 week follow-up period. The studies enrolled subjects with 4–8 clinically typical, visible, discrete AK lesions within a 25cm2 contiguous treatment area. Hypertrophic and hyperkeratotic lesions were excluded. On each dosing day, gel was applied to the entire treatment area. Efficacy was assessed at Day 57. Complete clearance rate was defined as the proportion of subjects with no (zero) clinically visible AK lesions in the treatment area. Partial clearance rate was defined as the proportion of subjects with ≥75% reduction in the number of AK lesions at baseline in the selected treatment area. In Study 1, the complete clearance rate for Picato was 37% and vehicle was 2%; partial clearance rate for Picato was 60% and vehicle was 7%. In Study 2, the complete clearance rate for Picato was 47% and vehicle was 5%; partial clearance rate for Picato was 68% and vehicle was 8%.
In two other double-blind, vehicle-controlled clinical trials (Study 3 and Study 4), 458 adults with AK on the trunk or extremities were randomized to treatment with either Picato gel, 0.05% or vehicle gel for 2 consecutive days, followed by an 8 week follow-up period. The studies enrolled subjects with 4–8 clinically typical, visible, discrete AK lesions within a 25cm2 contiguous treatment area. Hypertrophic and hyperkeratotic lesions were excluded. On each dosing day, gel was applied to the entire treatment area. In Study 3, at Day 57, the complete clearance rate for Picato was 28% and vehicle was 5%; partial clearance rate for Picato was 44% and vehicle was 7%. In Study 4, the complete clearance rate for Picato was 42% and vehicle was 5%; partial clearance rate for Picato was 55% and vehicle was 7%.
Subjects who achieved complete clearance at Day 57 in Study 1, 2, and 4 entered a 12-month follow-up period.
Legal Classification:
Rx
Adults:
For topical use only; not for oral, ophthalmic, or intravaginal use. Face and scalp: apply 0.015% gel to the affected area once daily for 3 consecutive days. Trunk and extremities: apply 0.05% gel to the affected area once daily for 2 consecutive days. Limit application to one contiguous skin area of approximately 25cm2 using one unit dose tube. Allow treated area to dry for 15 minutes after application. Wash hands immediately after application; avoid inadvertent transfer of drug to other areas (eg, eyes). Avoid washing and touching treated area for 6 hours after application; following this time, may wash with mild soap.
Children:
<18yrs: not established.
Warnings/Precautions:
Eye disorders (eg, severe eye pain, eyelid edema, eyelid ptosis, periorbital edema) may occur after exposure. Avoid contact with the periocular area. Administration not recommended until skin is healed from previous drug or surgical treatment. Severe skin reactions. Pregnancy (Cat. C). Nursing mothers.
Adverse Reaction(s):
Local skin reactions (eg, erythema, crusting, swelling, vesiculation/pustulation, erosion/ulceration), application site pain/pruritus/irritation/infection, periorbital edema, nasopharyngitis, headache.
How Supplied:
Single-use tubes 0.015%—3
0.05%—2
Last Updated:
3/2/2012