近日，美国食品和药物管理局（FDA）批准Picato（ingenol mebutate）凝胶（0.015％，0.05％）用于光化性角化病的局部治疗（AK）。AK是由累积的阳光暴露引起的癌前病变，其可能发展成鳞状细胞癌（SCC），这是第二种最常见的皮肤癌类型。
每天一次在脸部和头皮上使用Picato®0.015％凝胶连续三天，并且每天在躯干和四肢上使用Picato®0.05％凝胶连续两天。
Picato®凝胶是第一种也是唯一一种可以使用两到三天的局部AK疗法。
批准日期：2012年1月25日 公司：LEO制药
PICATO（巨大戟醇酯[ingenol mebutate]）凝胶，局部使用0.015％
PICATO（巨大戟醇酯[ingenol mebutate]）凝胶，局部使用0.05％
美国首次批准：2012
目前的主要变化
剂量和给药方法...........................10/2015
禁忌.....................................10/2015
警告和注意事项，眼部的不良反应...........10/2015
警告和注意事项，过敏反应.................10/2015
作用机制
不知道PICATO®凝胶在治疗病变中诱导细胞死亡的作用机制
适应症和用法
Picato®凝胶是细胞死亡的用于局部治疗光化性角化病的指示的诱导剂。
用法用量
对于局部使用;不用于口服，眼，或阴道内的使用。
避免Picato®转移到眼周区域。
请不要选择靠近和周围的嘴和嘴唇的应用。
对于应用程序的使用一个单位剂量管约25厘米2（5厘米×5厘米）到一个连续的皮肤区域。
在面部或头皮光化性角化病：应用Picato凝胶，0.015％至患处，每天一次，连续3天。
在树干或四肢光化性角化病：应用Picato凝胶，0.05％，至患处，每日一次，连续2天。
剂型和规格
含有ingenol mebutate，0.015％或0.05％的凝胶
禁忌
已知过敏ingenol mebutate或制剂的任何成分。
警告和注意事项
避免在治疗眼周区域。眼部疾病，其中包括剧烈眼痛，化学性结膜炎，角膜烧伤，眼睑水肿，眼睑下垂，眶周水肿接触后可发生。避免意外转移的药物进入眼睛和眼周区域。如果发生意外暴露，用清水冲洗眼睛，并寻求医疗照顾。
局部皮肤反应可发生包括严重反应（如水疱/脓疱，糜烂/溃疡）。Picato®凝胶的管理，不推荐，直到皮肤从以前的任何药物或手术治疗痊愈。
不良反应
最常见的不良反应（≥2％）有局部皮肤反应，应用部位疼痛，应用部位瘙痒，应用场所刺激，应用部位感染，眶周水肿，鼻咽炎和头痛。
如何供应/贮存和处置
PICATO®凝胶是一种澄明无色凝胶和以单位剂量层压管供应含标示充填重量为0.47g, 可射出重量0.25g. 单次使用后应遗弃管。
可得到2种剂量强度的PICATO®凝胶：0.015%和0.05%：
剂量强度0.015%：每盒单位剂量管数3。NDC#50222-502-47
剂量强度0.05%：每盒单位剂量管数2。NDC#50222-503-47
PICATO®凝胶贮存在冰箱在36ºF–46ºF (2ºC–8ºC)；外出时允许32ºF–59ºF间(0ºC–15ºC) (见美国药典USP 对冷温控制)。保护不要冻结。
Picato(ingenol mebutate)gel, 0.015%, 0.05%
Indication
Picato(ingenol mebutate) gel, 0.015%, 0.05% is prescription medicine used on the skin to treat actinic keratosis.
Important Safety Information
Do not use Picato gel if you are allergic to ingenol mebutate or any of the ingredients in Picato® gel.
Eye problems, including severe eye pain, swelling or drooping of your eyelids, corneal burn, redness, swelling and irritation inside the eye, or swelling around your eyes can happen if Picato® gel gets in your eyes. To avoid getting any of the Picato® into or around the eyes, it is important that you wash your hands well with soap and water after applying Picato gel and be careful to keep Picato® gel on the treated area from coming into contact with your eyes. If you accidentally get Picato® gel in your eyes, flush them with large amounts of water and get medical care as soon as possible.
There have been reports of serious allergic reactions (hives, itching, flushing and swelling of the lips or tongue, trouble breathing or wheezing, chest tightness and dizziness or passing out) in patients using Picato. The frequency of these events or their relationship, if any, to treatment with Picato® is unknown. If you experience any such symptoms, discontinue Picato® immediately and seek emergency medical help.
For use on the skin only. Picato can be applied to a contiguous skin area of approximately 25 cm2(5cmx5cm). Do not use Picato in, around, or near your eyes, mouth, lips, or vagina.
Reports of hypersensitivity reactions(anaphylaxis and allergic contact dermatitis) and herpes zoster(shingles) have been received during post approval use of Picato®.
Severe skin reactions in the treated areas on the face/scalp and body/arms/legs, including redness, flaking or scaling, crusting, swelling, blisters, pus, ulcers or breakdown of your skin can happen after applying Picato®. You may also see changes in your skin color (pigmentation changes) and scarring where Picato® gel is applied. You should not use Picato® gel until your skin has healed from other treatments or surgeries. The most common side effects with Picato® gel on the face and scalp (≥2%) include skin reactions in the treatment area (94%), pain at the treatment area (15%), itching at the treatment area (8%), infection at the treatment area (3%), swelling around your eyelids (3%), and headache (2%).
The most common side effects with Picato® gel on the body, arms and legs (≥2%) include skin reactions in the treatment area (92%), itching at the treatment area (8%), skin irritation at the treatment area (4%), nose and throat irritation (2%), and pain at the treatment area (2%).
Tell your healthcare provider if you are pregnant or plan to become pregnant. It is not known if Picato® gel can harm your unborn baby.
It is also not known if Picato® is safe and effective for the treatment of actinic keratosis in children less than 18 years of age.