部份中文KEYTRUDA處方資料（僅供參考）
【藥物名】pembrolizumab
【商品名】KEYTRUDA
【最初獲批時間】2014年
【類別】單克隆抗體
【靶點】PD-1
【分子結構】
分子量為：149kDa
【生產公司】默克公司
【藥物成分】Pembrolizumab是一種人源化單克隆抗體，可以阻斷PD-1和它的配體PD-L1和PD-L2的相互作用。 Keytruda是一種無菌的、不含防腐劑、白色至灰白色的干凍粉，儲存在小瓶中，用於靜脈注射。每2毫升重建溶液包含50毫克Pembrolizumab，按配方製作含有組氨酸（3.1毫克）、聚山梨醇酯80（0.4毫克）、蔗糖（140毫克），且調整PH值到5.5。
Keytruda注射劑是一種無菌的、不含防腐劑、無色至乳白色的液體，儲存在小瓶中，用於靜脈注射。每毫升重建溶液包含25毫克Pembrolizumab，按配方製作含有組氨酸（1.55毫克）、聚山梨醇酯80（0.2毫克）、蔗糖（70毫克）、水。
【藥物機制】PD-1配體PD-L1、PD-L2與T細胞上的PD-1受體結合，從而抑制了T細胞增殖以及細胞因子分泌。 PD-1受體的上調會出現在某些腫瘤中，該通路傳導的信號可以抑制免疫T細胞監視作用的活化。 Pembrolizumab是一種單克隆抗體，可以與PD-1受體結合，從而阻斷其與配體PD-L1/2的相互作用，消除對PD-1通路介導的免疫應答的抑製作用。在同基因腫瘤小鼠模型中，阻斷PD-1活動可以達到減小腫瘤增長的作用。
【適應症】
1.黑素瘤
Keytruda用於治療不可切除或轉移性的黑素瘤患者。
2.非小細胞肺癌
Keytruda用於一線治療轉移性非小細胞肺癌，且患者PD-L1處於高表達水平[腫瘤佔比得分（TPS）大於50％]，EGFR或沒有ALK突變。
Keytruda用於治療TPS大於1％的轉移性非小細胞肺癌患者，且患者在鉑化療後出現了疾病進展。含有EGFR或ALK腫瘤基因畸變的患者在採用了FDA批准的治療後出現疾病進展。
3.頭頸癌
Keytruda用於治療復發性或轉移性頭頸鱗細胞癌患者，且患者在接受鉑化療後出現疾病進展。
4.經典型霍奇金淋巴瘤（復發或難治性）
治療難治性成人及兒童經典霍奇金淋巴瘤患者，或者接受3線以上治療後復發患者。
【劑量和藥物管理】
1.黑素瘤推薦劑量
靜脈注射的推薦劑量為每三週注射2毫克/千克Keytruda，注射時間超過30分鐘，直至出現疾病進展或不可耐受的藥物毒性。
2.非小細胞肺癌推薦劑量
靜脈注射的推薦劑量為每三週注射200毫克Keytruda，注射時間超過30分鐘，直至出現疾病進展或不可耐受的藥物毒性或者（無進展情況下）持續24個月。
3.頭頸鱗細胞癌推薦劑量
靜脈注射的推薦劑量為每三週注射200毫克Keytruda，注射時間超過30分鐘，直至出現疾病進展或不可耐受的藥物毒性或者（無進展情況下）持續24個月。
4.經典型霍奇金淋巴瘤
成人：靜脈注射的推薦劑量為每三週注射200毫克Keytruda，注射時間超過30分鐘，直至出現疾病進展或不可耐受的藥物毒性或者（無進展情況下）持續24個月。
兒童：2歲以上（含2歲）兒童及青少年：靜脈注射的推薦劑量為每三週注射2毫克/千克（最大劑量200mg），直至出現疾病進展或不可耐受的藥物毒性或者（無進展情況下）持續24個月。
5.劑量調整
暫停Keytruda：
2級肺炎、2級或3級結腸炎、3級或4級內分泌病、2級腎炎、天冬氨酸轉氨酶（AST）或丙氨酸轉氨酶（ALT）濃度是3-5倍正常值上限或總膽紅素含量在1.5-3倍正常值之間、任何其他嚴重或3級的治療引起的副作用。
出現以下情況時需要永久停止用藥
任何威脅到生命安全的副作用、3級或4級肺炎或2級嚴重性的複發性肺炎、3級或4級腎炎、AST或ALT要高於5倍正常值上限或總膽紅素高於3倍正常值上限、3級或4級輸注相關反應、持續性的2級或3級副反應且在最後一劑量的用藥12週後沒有緩解、任何3級副作用複發。
6、 製備與使用
Keytruda配備：
加入2.3毫升滅菌水，將水沿著瓶壁用注射管注入。緩慢旋轉小瓶，混合均勻。
【劑型和規格】
注射：50毫克乾凍粉儲存在一次性小瓶種，用於製作液體製劑。
液體製劑：100毫克/4毫升液體儲存在一次性小瓶中。靜置5分鐘消除氣泡，不要搖晃小瓶。
靜脈輸液準備：
配製前要視覺檢查液體有無雜質或變色。液體為無色至乳白色，若觀察到可見粒子，棄置藥物；稀釋Keytruda幹凍粉；從瓶中取出相應的Keytruda的量，然後轉移到放有生理鹽水的輸注包內，最終稀釋溶液的濃度為1毫克/毫升至10毫克/毫升。丟棄掉未使用的部分藥物。
【禁忌症】
無。
【警告和注意事項】
1.免疫介導性肺炎
Keytruda會引起免疫介導性肺炎，甚至出現致命的案例。監測患者是否出現肺炎的病症，使用放射影像技術對有疑似病症的患者進行檢測。出現2級以上肺炎，施用皮之類固醇（初始劑量為1毫克/千克/天，逐漸升至2毫克/千克/天）。
2.免疫介導性結腸炎
Keytruda會引起免疫介導性結腸炎，甚至出現致命的案例。監測患者是否出現結腸炎的病症。出現2級以上結腸炎，施用皮之類固醇（初始劑量為1毫克/千克/天，逐漸升至2毫克/千克/天）。
3.免疫介導性肝炎
Keytruda會引起免疫介導性肝炎，甚至出現致命的案例。監測患者是否出現肝炎的病症。出現2級以上肝炎，施用皮之類固醇（初始劑量為1毫克/千克/天，逐漸升至2毫克/千克/天）。
4.免疫介導性內分泌疾病
Keytruda會引起下垂體炎。監測患者是否出現下垂體炎的病症，根據情況施用皮之類固醇以及激素補充。
Keytruda會引起甲狀腺障礙。監測患者是否出現甲狀腺功能異常的病症，根據情況進行激素補充。
Keytruda會引起一型糖尿病，包括糖尿病酮酸症。監測患者是否出現高血糖症的病症，根據情況進行胰島素補充。
5.免疫介導性腎炎和腎功能障礙
Keytruda會引起免疫介導性腎炎，甚至出現致命的案例。監測患者是否出現腎功能障礙的症狀。出現2級以上腎炎，施用強的松（初始劑量為1毫克/千克/天，逐漸升至2毫克/千克/天）。
6.其他免疫介導性副反應
Keytruda會引起其他免疫介導性副反應。監測患者是否出現肝炎的病症，對於疑似症狀要確保採用合理的評估方法來確認病因並排除其他可能因素。根據副作用的嚴重程度，暫停Keytruda並施用皮之類固醇。
7.輸注反應
Keytruda會引起輸注反應，甚至出現致命的案例。監測患者是否出現輸注反應的病症（包括嚴格、發冷、氣喘、瘙癢、發紅、皮疹等）。出現3級以上輸注反應，停止注射並永久停藥。
8.胚胎毒性
基於作用機理，孕婦施用Keytruda會對胚胎造成傷害。
【不良反應】最常見的不良反應(≥20%的患者) 疲勞、瘙癢症、腹瀉、食慾下降、皮疹、呼吸困難、便秘、噁心。
【在特殊人群中的使用】
1.孕婦
基於作用機理，孕婦施用Keytruda會對胚胎造成傷害。單克隆抗體可以通過胎盤，因此pembrolizumab有可能通過母親轉移到發育的胎兒體內。目前尚無有效的人類數據顯示對胚胎的毒性。
2.哺乳
目前尚不知道pembrolizumab是否分泌進入乳汁，沒有相關研究顯示奶製品中Keytruda的影響或Keytruda會出現在乳汁中。但是由於很多藥物會分泌進入乳汁，因此告知患者在治療期間以及停藥後4個月內不要哺乳。
3.對生殖能力的影響
告知女患者在治療期間以及停藥後4個月內採取有效的避孕措施。
4.兒童使用
尚無建立兒童群體中Keytruda的安全性和有效性的研究。
5.老人使用
在臨床試驗中，沒有觀察到65歲以上患者和小於65歲患者用藥安​​全性和有效性的總體差異。
【藥物過量】目前尚無關於Keytruda過量的相關信息。
【藥品儲存】
儲存：
產品不含防腐劑。稀釋和配製的Keytruda溶液兩種方法：
1.室溫下，從配製開始不要超過6小時。
2.冰箱2°C 到 8°C，從配製開始不要超過24小時。
不要冷凍
施用：通過靜脈輸注線靜脈注射超過30分鐘，針頭0.2-5微米。不要用相同的輸注線輸注另外一種藥


Keytruda (Pembrolizumab for Injection)
KEYTRUDA is a prescription medicine used to treat:
•a kind of skin cancer called melanoma. It may be used when your melanoma has spread or cannot be removed by surgery (advanced melanoma).
•a kind of lung cancer called non–small cell lung cancer (NSCLC). ◦It may be used alone as your first treatment when your lung cancer has spread (advanced NSCLC) and tests positive for “PD-L1” and your tumor does not have an abnormal “EGFR” or “ALK” gene.
◦It may also be used alone for advanced NSCLC if you have tried chemotherapy that contains platinum and it did not work or is no longer working and your lung cancer tests positive for “PD-L1” and, if your tumor has an abnormal “EGFR” or “ALK” gene, you have also received an “EGFR” or “ALK” inhibitor medicine that did not work or is no longer working.
•a kind of cancer called head and neck squamous cell cancer (HNSCC). It may be used when your HNSCC has returned or spread and you have received chemotherapy that contains platinum and it did not work or is no longer working.
•a kind of cancer called classical Hodgkin lymphoma (cHL). KEYTRUDA may be used for cHL in adults and children when you have tried a treatment and it did not work or when your cHL has returned after you received 3 or more types of treatment.
•a kind of bladder or urinary tract cancer when it has spread or cannot be removed by surgery (advanced urothelial cancer) and you are not able to receive chemotherapy that contains a medicine called cisplatin, or you have received chemotherapy that contains platinum, and it did not work or is no longer working.
•a kind of cancer that is shown by a laboratory test to be a microsatellite instability-high (MSI-H) or a mismatch repair deficient (dMMR) solid tumor. KEYTRUDA may be used in adults and children to treat: ◦cancer that has spread or cannot be removed by surgery (advanced cancer), and
◦has progressed following treatment, and you have no satisfactory treatment options, or
◦you have colon or rectal cancer, and you have received chemotherapy with fluoropyrimidine, oxaliplatin, and irinotecan but it did not work or is no longer working.
It is not known if KEYTRUDA is safe and effective in children with MSI-H cancers of the brain or spinal cord (central nervous system cancers).
PD-L1 = programmed death ligand 1;
EGFR = epidermal growth factor receptor;
ALK = anaplastic lymphoma kinase.
Important Safety Information About KEYTRUDA® (pembrolizumab)
KEYTRUDA is a medicine that may treat certain cancers by working with your immune system. KEYTRUDA can cause your immune system to attack normal organs and tissues in any area of your body and can affect the way they work. These problems can sometimes become serious or life-threatening and can lead to death.
Call or see your doctor right away if you develop any symptoms of the following problems or these symptoms get worse:
Lung problems (pneumonitis). Symptoms of pneumonitis may include shortness of breath, chest pain, or new or worse cough.
Intestinal problems (colitis) that can lead to tears or holes in your intestine. Signs and symptoms of colitis may include diarrhea or more bowel movements than usual; stools that are black, tarry, sticky, or have blood or mucus; or severe stomach-area (abdomen) pain or tenderness.
Liver problems (hepatitis). Signs and symptoms of hepatitis may include yellowing of your skin or the whites of your eyes, nausea or vomiting, pain on the right side of your stomach area (abdomen), dark urine, feeling less hungry than usual, or bleeding or bruising more easily than normal.
Hormone gland problems (especially the thyroid, pituitary, adrenal glands, and pancreas). Signs and symptoms that your hormone glands are not working properly may include rapid heartbeat, weight loss or weight gain, increased sweating, feeling more hungry or thirsty, urinating more often than usual, hair loss, feeling cold, constipation, your voice gets deeper, muscle aches, dizziness or fainting, or headaches that will not go away or unusual headache.
Kidney problems, including nephritis and kidney failure. Signs of kidney problems may include change in the amount or color of your urine.
Skin problems. Signs of skin problems may include rash, itching, blisters, peeling or skin sores, or painful sores or ulcers in your mouth or in your nose, throat, or genital area.
Problems in other organs. Signs of these problems may include changes in eyesight, severe or persistent muscle or joint pains, severe muscle weakness, or low red blood cells (anemia), shortness of breath, irregular heartbeat, feeling tired, or chest pain (myocarditis).
Infusion (IV) reactions that can sometimes be severe and life-threatening. Signs and symptoms of infusion reactions may include chills or shaking, shortness of breath or wheezing, itching or rash, flushing, dizziness, fever, or feeling like passing out.
Rejection of a transplanted organ. People who have had an organ transplant may have an increased risk of organ transplant rejection if they are treated with KEYTRUDA.
Complications of stem cell transplantation that uses donor stem cells (allogeneic) after treatment with KEYTRUDA. These complications can be severe and can lead to death. Your doctor will monitor you for signs of complications if you are an allogeneic stem cell transplant recipient.
Getting medical treatment right away may help keep these problems from becoming more serious. Your doctor will check you for these problems during treatment with KEYTRUDA. Your doctor may treat you with corticosteroid or hormone replacement medicines. Your doctor may also need to delay or completely stop treatment with KEYTRUDA if you have severe side effects.
Before you receive KEYTRUDA, tell your doctor if you have immune system problems such as Crohn’s disease, ulcerative colitis, or lupus; have had an organ transplant; have lung or breathing problems; have liver problems; or have any other medical problems.
If you are pregnant or plan to become pregnant, tell your doctor. KEYTRUDA can harm your unborn baby. Females who are able to become pregnant should use an effective method of birth control during treatment and for at least 4 months after the final dose of KEYTRUDA. Tell your doctor right away if you become pregnant during treatment with KEYTRUDA.
If you are breastfeeding or plan to breastfeed, tell your doctor. It is not known if KEYTRUDA passes into your breast milk. Do not breastfeed during treatment with KEYTRUDA and for 4 months after your final dose of KEYTRUDA.
Tell your doctor about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.
Common side effects of KEYTRUDA include feeling tired, itching, diarrhea, decreased appetite, rash, fever, cough, shortness of breath, pain in muscles, bones or joints, constipation, and nausea.
In children, feeling tired, vomiting and stomach-area (abdominal) pain, and increased levels of liver enzymes and decreased levels of salt (sodium) in the blood are more common than in adults.
These are not all the possible side effects of KEYTRUDA.
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