Apatinib

Apatinib Mesylate

Apatinib mesylate is the first successful small-molecule tyrosine kinase inhibitor to be approved in gastric cancer (China, Dec 2014). In Europe and South Korea, it has been granted orphan drug designation and is soon expected the same in the US. It has been clinically tested with over 1,000 patients worldwide and has demonstrated efficacy in numerous cancers including gastric cancer, colorectal cancer, hepatocellular carcinoma, non-small cell lung cancer, esophageal cancer, thyroid cancer, mesothelioma, and neuroendocrine tumors. Apatinib mesylate has also shown potential to significantly improve outcomes in combination treatment with chemotherapeutics and immunotherapy, as well as for maintenance therapy.

For Patients

Apatinib is an oral anti-cancer compound being studied for its promising ability to fight solid cancers including late stage stomach cancer, colorectal cancer, and liver cancer. Although apatinib is already approved and marketed in China, it is not yet approved for patients in the rest of the world. Apatinib is available outside of China as an investigational drug, in a phase 3 clinical trial. Currently there are 95 medical centers and 12 countries in Asia, North America, and Europe that are actively enrolling patients. If you and your physician decide that this clinical trial may be the right option for you, you may contact the research staff listed in the trial listings at ClinicalTrials.gov #NCT03042611.

Clinical Trials

LSK BioPharma is currently conducting a global pivotal phase 3 trial of apatinib for patients with advanced or metastatic gastric cancer. The phase 3 trial is expected to enroll about 450 patients in 95 medical centers and 12 countries in Asia, North America, and Europe (NCT#03042611).  The Company is also initiating studies with apatinib in combination with immunotherapy.

LSK BioPharma has completed the phase 1/2a dose escalation and safety trial of apatinib. In this trial, apatinib demonstrated encouraging clinical benefit in study patients with advanced solid tumors, especially for gastric and colorectal cancer patients. Apatinib was well tolerated with rare incidence of grade 3/4 adverse events, with hypertension as the most significant adverse event.

Technical Description

Apatinib mesylate (YN968D1) is an orally bioavailable experimental drug candidate being developed outside of China by LSK BioPharma, for the treatment of solid tumors including advanced or metastatic gastric cancer, colorectal cancer, and hepatocellular carcinoma. YN968D1 was first synthesized and patented by Advenchen Laboratories in Southern California. Apatinib is currently marketed in China for advanced gastric cancer by the Chinese-territory license-holder, Jiangsu Hengrui Medicine Co., Ltd. LSK BioPharma holds the global rights (excluding China) and has partnered with Bukwang Pharmaceuticals Co., Ltd. for the development and marketing of apatinib in South Korea.

Apatinib is a selective potent inhibitor of vascular endothelial growth factor receptor-2 (known as VEGFR2) which mediates the primary pathway for tumor-mediated angiogenesis. It has been clinically tested in over 1,000 patients worldwide and has demonstrated efficacy in numerous cancers including gastric cancer, colorectal cancer, hepatocellular carcinoma, non-small cell lung cancer, esophageal cancer, thyroid cancer, mesothelioma, and neuroendocrine tumors. It has also shown potential to significantly improve outcomes in combination with chemotherapeutics and immunotherapy, as well as for maintenance therapy.

Reference

Salvage treatment with apatinib for advanced non-small-cell lung cancer.
OncoTargets and Therapy 2017

Randomized, Double-Blind, Placebo-Controlled Phase III
Trial of Apatinib in Patients With Chemotherapy-Refractory
Advanced or Metastatic Adenocarcinoma of the Stomach or
Gastroesophageal Junction. Journal of Clinical Oncology 2016

Apatinib — new third-line option for refractory gastric or GEJ cancer.
Nature Reviews Clinical Oncology 2016

Apatinib: A novel receptor tyrosine kinase inhibitor for the treatment
of gastric cancer. Cancer Letters 2016

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