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TUKYSA is indicated in combination with trastuzumab and capecitabine for treatment of adult patients with advanced unresectable or metastatic HER2-positive breast cancer, including patients with brain metastases, who have received one or more prior anti-HER2-based regimens in the metastatic setting.
重要的安全信息
腹泻: TUKYSA can cause severe diarrhea including 脱水, hypotension, acute kidney injury, and death. 在HER2CLIMB, 81% of patients who received TUKYSA experienced diarrhea, including 12% with Grade 3 and 0.5% 4级. Both patients who developed Grade 4 diarrhea subsequently died, with diarrhea as a contributor to death. Median time to onset of the first episode of diarrhea was 12 days and the median time to resolution was 8 days. 腹泻导致了TUKYSA 剂量减少 6%的病人 TUKYSA 停药 in 1% of patients. Prophylactic use of antidiarrheal treatment was not required on HER2CLIMB.
If diarrhea occurs, administer antidiarrheal treatment as clinically indicated. Perform diagnostic tests as clinically indicated to exclude other causes of diarrhea. Based on the severity of the diarrhea, 中断剂量, then dose reduce or permanently discontinue TUKYSA.
肝毒性: TUKYSA can cause severe 肝毒性. 在HER2CLIMB, 8% of patients who received TUKYSA had an ALT increase >5 × ULN, 6% had an AST increase >5 × ULN, and 1.5% had a bilirubin increase >3 × ULN (Grade ≥3). Hepatotoxicity led to TUKYSA 剂量减少s in 8% of patients and TUKYSA 停药 in 1.5%的病人.
监控管理, AST, and bilirubin prior to starting TUKYSA, every 3 weeks during treatment, 正如临床所示. Based on the severity of hepatoxicity, 中断剂量, then dose reduce or permanently discontinue TUKYSA.
Embryo-Fetal毒性: TUKYSA会对胎儿造成伤害. Advise pregnant women and females of reproductive potential 潜在的 对胎儿的风险. Advise females of reproductive potential, and male patients with female partners of reproductive potential, to use effective contraception during TUKYSA treatment and for at least 1 week after the last dose.
Serious adverse reactions occurred in 26% of patients who received TUKYSA; those occurring in ≥2% of patients were diarrhea (4%), 呕吐(2.5%), 恶心想吐 (2%), 腹部疼痛 (2%), and seizure (2%). Fatal adverse reactions occurred in 2% of patients who received TUKYSA including sudden death, 脓毒症, 脱水, 、心原性休克.
Adverse reactions led to treatment 停药 in 6% of patients who received TUKYSA; those occurring in ≥1% of patients were 肝毒性 (1.5%)和腹泻(1%). Adverse reactions led to 剂量减少 in 21% of patients who received TUKYSA; those occurring in ≥2% of patients were 肝毒性 (8%) and diarrhea (6%).
The most common adverse reactions in patients who received TUKYSA (≥20%) were diarrhea, palmar-plantar erythrodysesthesia, 恶心想吐, 乏力, 肝毒性, 呕吐, 口腔炎, 食欲下降, 腹部疼痛, 头疼, 贫血, 和皮疹.
在HER2CLIMB, Grade ≥3 laboratory abnormalities reported in ≥5%的病人 who received TUKYSA were decreased phosphate, 增加ALT, 减少钾, 和增加AST.
The mean increase in serum creatinine was 32% within the first 21 days of treatment with TUKYSA. The serum creatinine increases persisted throughout treatment and were reversible upon treatment completion. Consider alternative markers of renal function if persistent elevations in serum creatinine are observed.
Strong CYP3A/中度:CYP2C8诱发者 Concomitant use may decrease TUKYSA activity. Avoid concomitant use of TUKYSA.
Strong or Moderate CYP2C8 Inhibitors: Concomitant use of TUKYSA with a strong CYP2C8 inhibitor may increase the risk of TUKYSA toxicity; avoid concomitant use. Increase monitoring for TUKYSA toxicity with moderate CYP2C8 inhibitors.
CYP3A基质: Concomitant use may increase the toxicity associated with a CYP3A 底物. Avoid concomitant use of TUKYSA where minimal concentration changes may lead to serious or life-threatening toxicities. If concomitant use is unavoidable, decrease the CYP3A 底物 dosage.
P-gp 基板: Concomitant use may increase the toxicity associated with a P-gp 底物. Consider reducing the dosage of P-gp 底物s where minimal concentration changes may lead to serious or life-threatening toxicity.
哺乳期: Advise women not to breastfeed while taking TUKYSA and for at least 1 week after the last dose.
肾功能损害: Use of TUKYSA in combination with capecitabine and trastuzumab is not recommended in patients with severe renal impairment (CLcr < 30 mL/min), because capecitabine is contraindicated in patients with severe renal impairment.
肝损伤: Reduce the dose of TUKYSA for patients with severe (Child-Pugh C) hepatic impairment.
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