Poster Includes Preclinical Data on Pan-RAS Compounds Demonstrating Inhibition in Breast Cancer Models
CARLSBAD, Calif., Oct. 23, 2023 (GLOBE NEWSWIRE) -- Qualigen Therapeutics, Inc. (Nasdaq: QLGN), a clinical-stage therapeutics company focused on developing treatments for adult and pediatric cancers with potential for Orphan Drug Designation, today announces a poster presentation on the Company's Pan-RAS platform at the American Association for Cancer Research (AACR) Special Conference in Breast Cancer Research, held October 19th to 22nd at the Westin San Diego Bayview.
"The RAS pathway continues to be an area of immense interest within the scientific community and biopharmaceutical industry. Due to the prevalence and severity of RAS-driven tumors, there is a high unmet need to discover and develop more broadly acting RAS-targeted compounds. We believe a pan-RAS approach may potentially overcome KRAS G12C resistance that affects depth and duration of responses of emerging therapies," commented Michael Poirier, Qualigen's Chairman and CEO. "We are grateful for our partnership with Dr. Geoff Clark and his team at the University of Louisville, who have demonstrated the therapeutic potential of our approach to RAS."
RAS is seldom mutated in breast cancer, but it is often hyperactivated by upregulation of positive regulator activity (such as Her-2) or down-regulation of negative regulator activity (such as NF1 or DAB2IP). These effects are particularly common in Luminal B breast cancer. As a result, we have developed a series of novel direct Pan-RAS inhibitors that exhibit a distinct binding mechanism to other currently described RAS inhibitors.
Poster highlights included:
Our RAS inhibitors suppressed the interaction of RAS with its downstream mitogenic effectors and suppressed RAS signaling pathways (MAPK and RAL pathways) in Luminal B breast cell model systems.
Our Pan-RAS compounds inhibited 3D growth at doses that have little effect on normal 2D growth and are active against in vivo xenograft breast tumors and can be orally available.
Abstract #: | B020 |
Title: | "Pan-RAS Inhibitors to Treat Luminal B Breast Cancer" |
Author/s: | Geoff Clark, Ph.D., et. al. |
Presentation Date: | October 21, 2023 5:00 to 7:00pm PT |
Location | Westin San Diego Bayview |
RAS is the most common cancer oncogene. Activating mutations in one of the three human RAS gene isoforms (KRAS, HRAS, or NRAS) are present in about one-fourth of all cancers. For example, mutant KRAS is found in 98% of pancreatic ductal adenocarcinomas, 52% of colon cancers, and 32% of lung adenocarcinomas. According to the National Cancer Institute, mutant KRAS subsets of these three cancers alone are diagnosed in more than 170,000 people each year in the United States, resulting in more than 120,000 deaths annually.1 Substantial scientific and pharmaceutical industry interest is evident by the compounds either approved or in development to treat devastating RAS-driven advanced solid tumors, such as pancreatic cancer.
About Pan-RAS
Qualigen Therapeutics is collaborating with Dr. Geoff Clark and Dr. Joe Burlison at the University of Louisville, Kentucky to develop a series of potentially highly potent compounds to take forward into preclinical development. Lead compounds are believed to suppress or block the interaction of endogenous RAS with c-RAF, and thereby influence the KRAS, HRAS, and NRAS effector pathways. RAS acts as a "hub" that activates multiple effector pathways, hence blocking any single pathway may be ineffective for many RAS-driven tumor types, including pancreatic, lung, and colorectal cancers. This approach could potentially enable a differentiated, pan-RAS strategy for inhibiting the MAPK, PI3K, and RAL pathways implicated in cancer cell proliferation, survival, and differentiation.
About Qualigen Therapeutics, Inc.
Qualigen Therapeutics, Inc. is a clinical-stage therapeutics company focused on developing treatments for adult and pediatric cancer. Our investigational QN-302 compound is a small molecule selective transcription inhibitor with strong binding affinity to G4s prevalent in cancer cells; such binding could, by stabilizing the G4s against "unwinding," help inhibit cancer cell proliferation. The investigational compounds within Qualigen's family of Pan-RAS oncogene protein-protein interaction inhibitor small molecules are believed to block the binding of mutated RAS proteins to their effector proteins, thereby leaving the mutated RAS unable to cause further harm. In theory, such mechanism of action may be effective in the treatment of about one quarter of all cancers, including certain forms of pancreatic, colorectal, and lung cancers.
Contact:
Investor Relations
ir@qlgntx.com
Source: Qualigen Therapeutics, Inc.
海報包括Pan-ras化合物的臨床前數據,這些化合物在乳腺癌模型中表現出抑制作用
加利福尼亞州卡爾斯巴德,2023年10月23日(GLOBE NEWSWIRE)——Qualigen Therapeutics, Inc.(納斯達克股票代碼:QLGN)是一家專注於開發可能獲得孤兒藥認定的成人和兒科癌症治療方法的臨床階段治療公司,今天宣佈在10月19日舉行的美國癌症研究協會(AACR)乳腺癌研究特別會議上在該公司的泛Ras平台上發佈海報第 22 名在聖地亞哥灣景威斯汀酒店。
“RAS 途徑仍然是科學界和生物製藥行業非常感興趣的領域。由於RAS驅動的腫瘤的患病率和嚴重程度,發現和開發作用更廣泛的RAS靶向化合物的需求很高,但尚未得到滿足。我們認爲,泛RAS方法有可能克服影響新興療法反應深度和持續時間的KRAS G12C耐藥性。” Qualigen董事長兼首席執行官邁克爾·普瓦里爾評論說。“我們感謝我們與傑夫·克拉克博士及其在路易斯維爾大學的團隊的合作,他們已經證明了我們治療急性呼吸道炎的方法具有治療潛力。”
RAS 在乳腺癌中很少發生突變,但它通常會因上調陽性調節活性(例如 Her-2)或下調陰性調節劑活性(例如 NF1 或 DAB2IP)而過度激活。這些影響在 Luminal B 乳腺癌中尤爲常見。因此,我們開發了一系列新型的直接泛RAS抑制劑,這些抑制劑與目前描述的其他RAS抑制劑具有獨特的結合機制。
海報亮點包括:
我們的 RAS 抑制劑抑制了 RAS 與其下游有絲分裂效應因子的相互作用,抑制了 Luminal B 乳腺細胞模型系統中的 RAS 信號通路(MAPK 和 RAL 通路)。
我們的Pan-ras化合物抑制了三維生長,其劑量對正常的二維生長影響不大,並且對體內異種移植乳腺腫瘤具有活性,並且可以口服。
摘要 #: | B020 |
標題: | “Pan-ras 抑制劑用於治療 Luminal B 型乳腺癌“ |
作者/s: | 傑夫·克拉克博士,等 |
演示日期: | 太平洋時間 2023 年 10 月 21 日下午 5:00 至晚上 7:00 |
地點 | 聖地亞哥灣景威斯汀酒店 |
RAS 是最常見的癌症癌基因。大約四分之一的癌症中存在三種人類 RAS 基因亞型(KRAS、HRAS 或 NRAS)之一的激活突變。例如,在98%的胰腺導管腺癌、52%的結腸癌和32%的肺腺癌中發現了突變的KRAS。根據美國國家癌症研究所的數據,僅這三種癌症的突變KRAS子群在美國每年就有超過17萬人被診斷出來,每年導致超過12萬人死亡。1 已獲批准或正在開發的用於治療毀滅性RAS驅動的晚期實體瘤(例如胰腺癌)的化合物顯然引起了科學和製藥業的極大興趣。
關於 Pan-ras
Qualigen Therapeutics正在與肯塔基州路易斯維爾大學的傑夫·克拉克博士和喬·伯裏森博士合作開發一系列潛在的高效化合物,以推進臨床前開發。據信,鉛化合物可以抑制或阻斷內源性 RAS 與 c-raf 的相互作用,從而影響 KRAS、HRAS 和 NRAS 效應器通路。RAS 充當激活多種效應器通路的 “樞紐”,因此阻斷任何單一途徑可能對許多 RAS 驅動的腫瘤類型無效,包括胰腺癌、肺癌和結直腸癌。這種方法有可能實現一種差異化的泛RAS策略,以抑制與癌細胞增殖、存活和分化相關的MAPK、PI3K和RAL途徑。
關於 Qualigen Therapeutics, Inc.
Qualigen Therapeutics, Inc. 是一家臨床階段的治療公司,專注於開發成人和兒童癌症的治療方法。我們正在研究的 QN-302 化合物是一種小分子選擇性轉錄抑制劑,對癌細胞中普遍存在的 G4 具有很強的結合親和力;這種結合可以通過穩定 G4 免受 “鬆開” 來幫助抑制癌細胞的增殖。據信,Qualigen的Pan-ras癌基因蛋白質相互作用抑制劑小分子家族中的研究化合物可以阻斷突變的RAS蛋白與其效應蛋白的結合,從而使突變的RAS無法造成進一步的傷害。從理論上講,這種作用機制可以有效治療大約四分之一的癌症,包括某些形式的胰腺癌、結直腸癌和肺癌。
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投資者關係
ir@qlgntx.com
資料來源:Qualigen Therapeutics