Takeda’s EXKIVITY® (mobocertinib) Receives Approval from the NMPA of China, Becoming the First and Only Therapy Available for Patients with EGFR Exon20 Insertion+ NSCLC
– EXKIVITY is the First Category-1 Innovative Drug Approved for Takeda China Following a Phase 2 Global Pivotal Study
– Approval Based on Data from the Phase 1/2 Clinical Trial Demonstrating EXKIVITY’s Clinical Benefit and Durable Responses in EGFR Exon20 Insertion+ NSCLC
– Results Demonstrated a Confirmed Overall Response Rate (ORR) of 28% and Median Duration of Response (DoR) of 15.8 Months per Independent Review Committee (IRC)
“The approval of EXKIVITY in
Lung cancer is the most commonly diagnosed cancer in
“Since the discovery of EGFR mutations nearly twenty years ago, patients with Exon20 insertions have been waiting for a targeted therapy to treat their disease,” said
This approval is based on the results from the platinum-pretreated population in the Phase 1/2 trial of EXKIVITY, which consisted of 114 patients with EGFR Exon20 insertion+ NSCLC
About EXKIVITY (mobocertinib)
EXKIVITY is a first-in-class, oral tyrosine kinase inhibitor (TKI) specifically designed to selectively target epidermal growth factor receptor (EGFR) Exon20 insertion mutations.
EXKIVITY is currently approved in
For more information about EXKIVITY, visit https://www.exkivity.com/. For the Prescribing Information, including the Boxed Warning, please visit https://takeda.info/Exkivity-Prescribing-Information.
About EGFR Exon20 Insertion+ NSCLC
Non-small cell lung cancer (NSCLC) is the most common form of lung cancer, accounting for approximately 85% of the estimated 2.2 million new cases of lung cancer diagnosed each year worldwide, according to the
Takeda is committed to continuing research and development to meet the needs of the lung cancer community through the discovery and delivery of transformative medicines.
EXKIVITY IMPORTANT SAFETY INFORMATION
QTc Interval Prolongation
Heart rate-corrected QT (QTc) interval prolongation, including resultant life-threatening arrhythmias, such as Torsades de Pointes, occurred in patients treated with mobocertinib.
A concentration-dependent QTc interval prolongation of approximately 12.7 msec (90% CI: 8.69, 16.8) was observed at the steady-state Cmax following 160 mg daily doses based on an analysis of data from 194 patients with advanced solid malignances.
Clinical trials of mobocertinib did not enroll patients with baseline QTc greater than 470 msec. Assess QTc and electrolytes at baseline and correct abnormalities in sodium, potassium, calcium, and magnesium prior to initiating mobocertinib. Monitor QTc and electrolytes periodically during treatment. Increase monitoring frequency in patients with risk factors for QTc prolongation, such as in patients with congenital long QTc syndrome, heart disease, electrolyte abnormalities, or those
Interstitial Lung Disease/Pneumonitis
Severe, life-threatening, and fatal interstitial lung disease (ILD)/pneumonitis have occurred in patients treated with mobocertinib.
Withhold mobocertinib for acute onset of new or progressive unexplained pulmonary symptoms such as dyspnea, cough, and fever pending diagnostic evaluation and diagnosis confirmation. Permanently discontinue mobocertinib if ILD/pneumonitis is confirmed.
Cardiac failure (including congestive cardiac failure, decreased ejection fraction, and cardiomyopathy) has occurred in patients treated with mobocertinib.
Mobocertinib can cause QTc prolongation resulting in Torsades de Pointes.
Atrial fibrillation (1.3%), ventricular tachycardia (0.3%), first degree atrioventricular block (0.7%), second degree atrioventricular block (0.3%), left bundle branch block (0.3%), supraventricular extrasystoles (0.3%) and ventricular extrasystoles (0.3%) also occurred in patients receiving mobocertinib. The causality of these events to mobocertinib has not been established.
Conduct cardiac monitoring, including assessment of left ventricular ejection fraction at baseline and during treatment. Patients
In clinical studies, most patients experienced mild to moderate diarrhea. Diarrhea can be severe or life threatening. The median time to first onset of diarrhea was five days but could occur as soon as 24 hours after administration of mobocertinib. Diarrhea is usually transient and had a median time to resolution of three days. Prolonged diarrhea may lead to dehydration or electrolyte imbalance, with or without renal impairment.
Early and compliant diarrhea management such as prescribed anti-diarrheal medicinal products (e.g., loperamide), diet, adequate fluid intake (~2L clear liquids per day), and patient education is recommended. Instruct patients to have anti-diarrheal medicinal products (e.g., loperamide) readily available. Begin anti-diarrheal treatment at the first episode of poorly formed or loose stools or the earliest onset of bowel movements more frequent than normal. In mobocertinib clinical trials where loperamide was used as the antidiarrheal, the dosage regimen for loperamide was 4 mg at the first bout of diarrhea and then 2 mg every 2 hours until the patient is diarrhea-free for at least 12 hours; daily dose of loperamide did not exceed 16 mg. If using loperamide as the antidiarrheal treatment, refer to loperamide product labeling for additional information.
If diarrhea does not improve or additional signs or symptoms are reported, standard medical practice intervention, including other anti-diarrheal medications, are recommended. Antidiarrheal prophylaxis may be considered as needed. Monitor electrolytes and instruct patients to increase fluid and electrolyte intake as needed. No dose modification is necessary unless the patient does not tolerate mobocertinib or the symptoms recur, or the diarrhea doesn’t resolve with medical intervention. Interrupt mobocertinib and reduce subsequent doses if severe diarrhea occurs.
Based on its mechanism of action and data from animal studies, mobocertinib can cause fetal harm when administered to pregnant women.
Advise pregnant women of the potential risk to a fetus. Advise females of reproductive potential to use effective non-hormonal contraception during treatment with mobocertinib and for one month following the final dose. Advise males with female partners of reproductive potential to use effective contraception during treatment with mobocertinib and for one week following the final dose of mobocertinib.
Takeda’s Commitment to Oncology
At Takeda Oncology, we are united by our aspiration to cure cancer and motivated every day to work harder for patients with limited or ineffective treatment options. Our agile structure and deep in-house expertise are complemented by a network of partnerships that optimize our ability to research, develop and deliver transformative medicines to people living with cancer. Building on decades of leadership in oncology and a portfolio of approved medicines for hematologic cancers and solid tumors, we are advancing a cutting-edge pipeline focused on the power of innate immunity. With inspiration from patients and innovation from everywhere, our goal is to introduce new classes of immunotherapies that can lead to deep, durable responses so that more patients can benefit from – and have access to – innovative medicines.
For more information, visit www.takedaoncology.com.
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This indication is approved in
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