Antengene Announces Dosing of First Patient in the ATG-019 (KPT-9274) Phase 1 Trial, a First-in-Class Dual Inhibitor, for Advanced Solid Tumors and Non-Hodgkin’s Lymphoma

Press release content from PR Newswire. The AP news staff was not involved in its creation.

SHANGHAI and PHILADELPHIA, April 14, 2020 /PRNewswire/ — Antengene announced today that it has dosed the first patient in Taiwan, China in its phase 1 open-label clinical trial of ATG-019 (KPT-9274), a dual inhibitor of both PAK4 and NAMPT. This trial is being conducted to evaluate the safety and tolerability of ATG-019 monotherapy or ATG-019 combined with niacin ER (vitamin B3/nicotinic acid), for the treatment of advanced solid tumors or non-Hodgkin’s lymphoma.

ATG-019 is a first-in-class, also the only orally bioavailable dual-target inhibitor targeting both p21-activated kinase 4 (PAK4) and nicotinamide phosphoribosyl transferase (NAMPT). PAK4 regulates numerous fundamental cellular processes, including intracellular transport, cellular division, cell shape and motility, immune defense and the development of cancer. PAK4 interacts with many key signaling molecules involved in cancer development such as beta-catenin, CDC42, Raf-1, BAD and myosin light chain. The overexpression and overactivation of PAK4 lead to tumor proliferation and metastasis and show a negative correlation with the infiltration of immune cells, leading to tumor proliferation and metastasis. NAMPT is the rate-limiting enzyme in the metabolic scavenging pathway that utilizes nicotinamide to replenish nicotinamide adenine dinucleotide (NAD), an essential metabolic cofactor and second messenger. Inhibition of NAMPT can effectively inhibit the energy metabolism and growth of tumor cells.

In May 2018, Antengene entered into a broad strategic collaboration with Karyopharm Therapeutics Inc. (Nasdaq: KPTI) and obtained exclusive rights for development and commercialization of four clinical stage, novel, oral drug candidates, including KPT-9274 (ATG-019), in various Asian countries and regions. As an oral small molecule inhibitor with the novel mechanism with novel targets, ATG-019 inhibits the occurrence, development, invasion and migration of tumors through the precise targeting and inhibiting both PAK4 and NAMPT. Preclinical studies has demonstrated the significant inhibitory effect of ATG-019 on multiple tumors types including lung cancer, multiple myeloma, leukemia, and lymphoma, etc.

“We are pleased that the first patient of ATG-019 was successfully enrolled and dosed. This is our first step in developing PAK4/NAMPT dual-target inhibitor,” said Dr. Jay Mei, founder, chairman and CEO of Antengene. “In addition to conducting the clinical trial for the treatment of advanced solid tumors and non-Hodgkin’s lymphoma, Antengene is also exploring the potential for ATG-019 in the treatment of different indications and in combination with existing regimens based on the anti-proliferative activity of ATG-019 on cancer cells. We hope to explore its potential from multiple dimensions in the near future.”

About Antengene

Antengene is a China-and-U.S. based biopharmaceutical company focusing on drug discovery, clinical development and the commercialization of innovative therapeutics to meet unmet medical needs. Antengene aims to provide the most advanced and first-in-class anti-cancer drugs and other treatments for patients in China, Asia and around the world. In April 2017, Celgene (now officially acquired by Bristol-Myers Squibb, and become the world’s top ten pharmaceutical company after the merge), a global leading innovative biopharmaceutical company became a long-term strategic partner and obtained an equity position in Antengene. In January 2020, former Celgene chairman and CEO Mark J. Alles joined Antengene Board of Directors and former Celgene China GM John Chin joined the company as Chief Business Officer.

At present, Antengene’s pipeline includes six clinical stage products:

ATG-010 (selinexor) is the first oral selective inhibitor of nuclear export compound with novel mechanisms in the world. On July 3, 2019, the U.S. FDA approved ATG-010 in combination with low-dose dexamethasone for the treatment of adult patients with relapsed refractory multiple myeloma. Currently, the registered clinical trials of ATG-010 in relapsed refractory multiple myeloma (RRMM) and diffuse large B-cell lymphoma (DLBCL) is ongoing in China. The compound is also in late clinical development and the stage of registered clinical trials for various other hematologic malignancies and solid tumors. In addition, preclinical studies have shown that inhibitors of nuclear protein export can effectively treat a wide range of tumors carrying KRAS mutation, and related clinical studies have been conducted recently; ATG-008 is a second-generation dual mTORC1/2 inhibitor and is in a multi-regional clinical trial for treatment of advanced liver cancer, lung cancer, and several other tumors, including in combination with anti-PD-1 antibody; ATG-016 is a second-generation oral selective inhibitor of nuclear export protein, and is currently being studied in myelodysplastic syndrome (MDS) as well as in several clinical trials of solid tumors, including colorectal cancer (CRC), gastric carcinoma (GC), triple-negative breast cancer (TNBC) and prostate cancer (PrC); ATG-019 is the first-in-class PAK4/NAMPT dual-target inhibitors, and is currently been studied in a number of clinical trials including non-Hodgkin’s lymphoma (NHL), colorectal cancer, lung cancer, and melanoma. In addition, preclinical studies have demonstrated that ATG-019 in combination with anti-PD-1 antibodies can effectively improve the anti-tumor activity and is effective in patients who acquire resistance to anti-PD-1 therapy. Related clinical trial is about to initiate; ATG-527 is an innovative product under development for antiviral and treatment of autoimmune diseases, and has been in clinical trials conducted in Epstein-Barr virus (EBV), respiratory syncytial virus (RSV) infection, cytomegalovirus (CMV) infection and Systemic lupus erythematosus (SLE) and other related diseases; ATG-017 is a potent and selective small molecule extracellular signal–regulated kinases 1 and 2 (ERK1/2) inhibitor, in clinical development for the treatment of various solid tumors, non-Hodgkin’s lymphoma, acute myelocytic leukemia (AML) and multiple myeloma. In addition, the drug discovery team of Antengene focuses on the early preclinical development of multiple innovative target drugs in the fields of small molecule, monoclonal and bi-specific antibodies.

View original content:[1]

SOURCE Antengene Corporation

Source URL: Read More
The public content above was dynamically discovered – by graded relevancy to this site’s keyword domain name. Such discovery was by systematic attempts to filter for “Creative Commons“ re-use licensing and/or by Press Release distributions. “Source URL” states the content’s owner and/or publisher. When possible, this site references the content above to generate its value-add, the dynamic sentimental analysis below, which allows us to research global sentiments across a multitude of topics related to this site’s specific keyword domain name. Additionally, when possible, this site references the content above to provide on-demand (multilingual) translations and/or to power its “Read Article to Me” feature, which reads the content aloud to visitors. Where applicable, this site also auto-generates a “References” section, which appends the content above by listing all mentioned links. Views expressed in the content above are solely those of the author(s). We do not endorse, offer to sell, promote, recommend, or, otherwise, make any statement about the content above. We reference the content above for your “reading” entertainment purposes only. Review “DMCA & Terms”, at the bottom of this site, for terms of your access and use as well as for applicable DMCA take-down request.

Acquire this Domain
You can acquire this site’s domain name! We have nurtured its online marketing value by systematically curating this site by the domain’s relevant keywords. Explore our content network – you can advertise on each or rent vs. buy the domain. | Skype: TLDtraders | +1 (475) BUY-NAME (289 – 6263). Thousands search by this site’s exact keyword domain name! Most are sent here because search engines often love the keyword. This domain can be your 24/7 lead generator! If you own it, you could capture a large amount of online traffic for your niche. Stop wasting money on ads. Instead, buy this domain to gain a long-term marketing asset. If you can’t afford to buy then you can rent the domain.

About Us
We are Internet Investors, Developers, and Franchisers – operating a content network of several thousand sites while federating 100+ eCommerce and SaaS startups. With our proprietary “inverted incubation” model, we leverage a portfolio of $100M in valued domains to impact online trends, traffic, and transactions. We use robotic process automation, machine learning, and other proprietary approaches to power our content network. Contact us to learn how we can help you with your online marketing and/or site maintenance.