目前，默克发表的一项荟萃分析的结果显示：西妥昔单抗（爱必妥）联合以铂类为基础的标准一线化疗治疗非小细胞肺癌（NSCLC），与单用化疗药比较，在总生存期、无进展生存期和总有效率（总体生存期p=0.010；无进展生存期p=0.036；总有效率p<0.001）方面均有获益，爱必妥能够显著延长非小细胞肺癌患者的生存期，中位总生存期从10.1个月延长至11.3个月。在接受爱必妥治疗早期就出现痤疮样皮疹的患者中，这种延长生存的作用更加显著，中位总生存期达到了15个月。

最新研究显示，在接受西妥昔单抗治疗的患者当中，开始治疗3周以内出现皮疹（痤疮样皮疹）的患者的总生存期为15个月，而无皮疹的患者的总生存期为8.8个月。因此，对于接受西妥昔单抗联合化疗的患者，出现痤疮样皮疹与较好的预后相关。这提示，皮疹可能是生存期延长的一个重要指标。但专家同时指出，对没有出现皮疹的患者也应该坚持治疗，不要轻易放弃。

【商品名】爱必妥

【通用名】西妥昔单抗注射液

【英文商品名】Erbitux

【适应证】本品单用或与伊立替康(irinotecan)联用于表皮生长因子（EGF）受体过度表达的，对以伊立替康为基础的化疗方案耐药的转移性直肠癌的治疗。

【剂量用法】推荐起始剂量为400mg/m2，滴注时间120分钟，滴速应控制在5ml/min以内。维持剂量为一周250mg/m2，滴注时间不少于60分钟。提前给予H1受体阻断剂，对预防输液反应有一定作用。使用前勿振荡、稀释。

【不良反应】本品耐受性好，不良反应大多可耐受，最常见的是痤疮样皮疹、疲劳、腹泻、恶心、呕吐、腹痛、发热和便秘等。其他不良反应还有白细胞计数下降、呼吸困难等。皮肤毒性反应（痤疮样皮疹、皮肤干燥、裂伤和感染等）多数可自然消失。少数患者可能发生严重过敏反应、输液反应、败血症、肺间质疾病、肾衰、肺栓塞和脱水等。在接受本品单药治疗和本品与伊立替康联合治疗的患者中，分别为5%和10%的患者因不良反应退出。

【规格】100mg:50ml
【批准文号】S20050095

【生产厂家】德国默克Merck

Erbitux
Generic Name: cetuximab
Dosage Form: injection
FULL PRESCRIBING INFORMATION

WARNING: SERIOUS INFUSION REACTIONS and CARDIOPULMONARY ARREST Infusion Reactions: Serious infusion reactions occurred with the administration of Erbitux in approximately 3% of patients in clinical trials, with fatal outcome reported in less than 1 in 1000. [See Warnings and Precautions (5.1) and Adverse Reactions (6).] Immediately interrupt and permanently discontinue Erbitux infusion for serious infusion reactions. [See Warnings and Precautions (5.1) and Dosage and Administration (2.4).] Cardiopulmonary Arrest: Cardiopulmonary arrest and/or sudden death occurred in 2% of 208 patients with squamous cell carcinoma of the head and neck treated with radiation therapy and Erbitux. Closely monitor serum electrolytes, including serum magnesium, potassium, and calcium, during and after Erbitux. [See Warnings and Precautions (5.2, 5.6).]

1    INDICATIONS AND USAGE

1.1   Squamous Cell Carcinoma of the Head and Neck (SCCHN)

Erbitux® is indicated in combination with radiation therapy for the initial treatment of locally or regionally advanced squamous cell carcinoma of the head and neck. [See Clinical Studies (14.1).]

Erbitux, as a single agent, is indicated for the treatment of patients with recurrent or metastatic squamous cell carcinoma of the head and neck for whom prior platinum-based therapy has failed. [See Clinical Studies (14.1).]

1.2   Colorectal Cancer

Erbitux, as a single agent, is indicated for the treatment of epidermal growth factor receptor (EGFR)-expressing metastatic colorectal cancer after failure of both irinotecan- and oxaliplatin-based regimens. Erbitux, as a single agent, is also indicated for the treatment of EGFR-expressing metastatic colorectal cancer in patients who are intolerant to irinotecan-based regimens. [See Clinical Studies (14.2) and Warnings and Precautions (5.7).]

Erbitux, in combination with irinotecan, is indicated for the treatment of EGFR-expressing metastatic colorectal carcinoma in patients who are refractory to irinotecan-based chemotherapy. The effectiveness of Erbitux in combination with irinotecan is based on objective response rates. Currently, no data are available that demonstrate an improvement in disease-related symptoms or increased survival with Erbitux in combination with irinotecan for the treatment of EGFR-expressing, metastatic colorectal carcinoma. [See Clinical Studies (14.2) and Warnings and Precautions (5.7).]

 Retrospective subset analyses of metastatic or advanced colorectal cancer trials have not shown a treatment benefit for Erbitux in patients whose tumors had KRAS mutations in codon 12 or 13. Use of Erbitux is not recommended for the treatment of colorectal cancer with these mutations [see Clinical Studies (14.2) and Clinical Pharmacology (12.1).]

2    DOSAGE AND ADMINISTRATION

2.1   Squamous Cell Carcinoma of the Head and Neck

Erbitux in combination with radiation therapy:

• The recommended initial dose is 400 mg/m2 administered one week prior to initiation of a course of radiation therapy as a 120-minute intravenous infusion (maximum infusion rate 10 mg/min).
• The recommended subsequent weekly dose (all other infusions) is 250 mg/m2 infused over 60 minutes (maximum infusion rate 10 mg/min) for the duration of radiation therapy (6–7 weeks). Complete Erbitux administration 1 hour prior to radiation therapy.

Erbitux monotherapy:

• The recommended initial dose is 400 mg/m2 administered as a 120-minute intravenous infusion (maximum infusion rate 10 mg/min).
• The recommended subsequent weekly dose (all other infusions) is 250 mg/m2 infused over 60 minutes (maximum infusion rate 10 mg/min) until disease progression or unacceptable toxicity.

2.2   Colorectal Cancer

• The recommended initial dose, either as monotherapy or in combination with irinotecan, is 400 mg/m2 administered as a 120-minute intravenous infusion (maximum infusion rate 10 mg/min).
• The recommended subsequent weekly dose, either as monotherapy or in combination with irinotecan, is 250 mg/m2 infused over 60 minutes (maximum infusion rate 10 mg/min) until disease progression or unacceptable toxicity.

2.3   Recommended Premedication

Premedicate with an H1 antagonist (eg, 50 mg of diphenhydramine) intravenously 30–60 minutes prior to the first dose; premedication should be administered for subsequent Erbitux doses based upon clinical judgment and presence/severity of prior infusion reactions.

2.4   Dose Modifications

Infusion Reactions

Reduce the infusion rate by 50% for NCI CTC Grade 1 or 2 and non-serious NCI CTC Grades 3–4 infusion reactions.

Immediately and permanently discontinue Erbitux for serious infusion reactions requiring medical intervention and/or hospitalization. [See Warnings and Precautions (5.1).]

Dermatologic Toxicity

Recommended dose modifications for severe (NCI CTC Grade 3 or 4) acneform rash are specified in Table 1. [See Warnings and Precautions (5.4).]

Table 1: Erbitux Dose Modification Guidelines for Rash

Severe Acneform Rash	Erbitux	Outcome	Erbitux Dose Modification
1st occurrence	Delay infusion 1 to 2 weeks	Improvement	Continue at 250 mg/m2
		No Improvement	Discontinue Erbitux
2nd occurrence	Delay infusion 1 to 2 weeks	Improvement	Reduce dose to 200 mg/m2
		No Improvement	Discontinue Erbitux
3rd occurrence	Delay infusion 1 to 2 weeks	Improvement	Reduce dose to 150 mg/m2
		No Improvement	Discontinue Erbitux
4th occurrence	Discontinue Erbitux

2.5   Preparation for Administration

Do not administer Erbitux as an intravenous push or bolus.

Administer via infusion pump or syringe pump. Do not exceed an infusion rate of 10 mg/min.

Administer through a low protein binding 0.22-micrometer in-line filter.

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.

The solution should be clear and colorless and may contain a small amount of easily visible, white, amorphous, cetuximab particulates. Do not shake or dilute.