Latest clinical data from Entrectinib for NTRK1 / 2/3, ROS1 or ALK.

In September 2018 at the Canadian Cancer Research Association, the results of Phase I and Phase II clinical trials of the new drug entrectinib (code RXDX-101) positive non-small cell lung cancer (NSCLC) were presented and were very interesting.

Of the 53 evaluable patients, the response rate was 77.4% and the median response time was 24.6 months. It is worth mentioning that these patients included 20 of the untreated patients and 37% of the patients enrolled (37.7% of all registered patients) It was. The response rate was 55%.

ROS1 is a receptor tyrosine kinase that acts as an on / off switch for a variety of cellular functions. Under abnormal conditions, ROS1 is changed so that cells do not normally grow and grow, but the cells spread and survive, signaling that the cells become cancerous. ROS1 is present in 1% to 2% of patients with lung cancer.

Dr. Robert C. Doebele and colleagues say that entrectinib is superior to crizotinib as the first line of treatment for ROS1 + non-small cell lung cancer. Image from: University of Colorado Cancer Center

Dr. Doebele pointed out that one of the major differences between crizotinib and entrectinib clinical trials is that crizotinib does not usually penetrate the brain and central nervous system (CNS) and that entrectinib has potent CNS activity.

Conclusion

Entelelnib can treat existing central nervous system lesions across the blood-brain barrier, and can prevent or delay the onset of brain metastasis, a common site of progression, especially in NSCLC.

ROS1 fusion occurs in about 2% of non-small cell lung cancers, and CNS activity of entrectinib is an important difference of this compound because this compound tends to spread to the brain and can contribute to the proven impressive mitigation to date. Duration and progression free survival.

In addition to ROS1 - positive non - small cell lung cancer, entrectinib showed promising early antitumor activity in NTRK - positive solid tumors. Therefore, this drug has been approved by the US FDA's innovative treatment and European Medicines and Drug Administration (PRMA). The company has initiated a new drug application process for NTRK benign tumors and ROS1-positive non-small cell lung cancer therapies.

We hope that this drug will have good results in subsequent clinical trials and hope for early treatment of cancer patients.

Reference :

Https://ignyta.com/providers/rx-precision-medicine-pipeline/entrectinib/

Http://ntrkfusions.com/entrectinib-sensitivity-associated-with-a-novel-lmna-ntrk1-gene-fusion/

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4643748/

Https://medicalxpress.com/news/2018-09-phase-results-entrectinib-ros1-non-small.html