YL-17231 / Shanghai YingLi Pharma - LARVOL DELTA

Pan-RAS Inhibitor YL-17231 in Patients With Advanced Solid Tumors Harboring Mutations in KRAS, HRAS, or NRAS (clinicaltrials.gov) - P1 | N=60 | Recruiting | Sponsor: Shanghai YingLi Pharmaceutical Co. Ltd. | Not yet recruiting ➔ Recruiting | Trial primary completion date: Apr 2025 ➔ Oct 2025

Enrollment open • Trial primary completion date • Oncology • Solid Tumor • HRAS • KRAS • NRAS • PD-L1

280Bio doses first patient in Phase I clinical trial of TEB-17231, an oral pan-RAS inhibitor in patients with advanced cancers harboring mutations in KRAS, HRAS, or NRAS (PRNewswire) - "280Bio, Inc...today announced that the first patient was treated with TEB-17231 (YL-17231), a small molecule inhibitor of RAS signaling. 280Bio is a wholly owned subsidiary of Shanghai Yingli Pharmaceuticals, Inc. (Yingli Pharma) of Shanghai, China. KRAS, NRAS and HRAS genes are frequently mutated in many tumor indications causally associated with promoting tumor cell growth....'We look forward to continued enrollment and dosing of patients in this trial.'....This first US patient was enrolled at The University of Texas MD Anderson Cancer Center, Houston, Texas, by David Hong, MD, Deputy Chair of Investigational Cancer Therapeutics and lead investigator on the trial."

Enrollment status • Trial status • Oncology • Solid Tumor

Pan-RAS Inhibitor YL-17231 in Patients With Advanced Solid Tumors Harboring Mutations in KRAS, HRAS, or NRAS (clinicaltrials.gov) - P1 | N=60 | Not yet recruiting | Sponsor: Shanghai YingLi Pharmaceutical Co. Ltd.

Metastases • New P1 trial • Oncology • Solid Tumor • HRAS • KRAS • NRAS • PD-L1

A Study of YL-17231 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=80 | Recruiting | Sponsor: Shanghai YingLi Pharmaceutical Co. Ltd.

Metastases • New P1 trial • Colorectal Cancer • Gastrointestinal Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • KRAS • MSI • PD-L1

Yingli Pharmaceutical’s pan-KRAS mutation inhibitor is the first to be approved for clinical trials in the United States [Google translation] (Stockstar) - "On July 3, 2023, the new pan-KRAS mutation small molecule inhibitor drug independently developed by Shanghai Yingli Pharmaceutical Co., Ltd. was approved by the US FDA for clinical trials, and phase 1 clinical studies will be carried out in the United States in the near future....The clinically approved product is YL-17231, a pan-KRAS mutant oral small molecule inhibitor combined with the KRAS switch II pocket, jointly developed by Yingli Pharmaceutical and its wholly-owned subsidiary 280Bio...Next, 280Bio will join hands with Dr. David Hong, a world-renowned clinical oncology researcher at the University of Texas MD Anderson Cancer Center, to advance the Phase 1 clinical trial of YL-17231 and recruit subjects in the fourth quarter of this year."

IND • New P1 trial • Oncology • Solid Tumor

The small molecule KRAS inhibitor, TEB-17231, blocks tumor progression and overcomes KRASG12C inhibitor mediated resistance (AACR 2023) - "Further, TEB-17231 exhibited tumor growth inhibition (IC50) in KRAS-G12C Ba/F3 (14 nM) and derivative cell lines that acquired resistance to G12C inhibitor MRTX849 by the additional KRAS domain mutations as follows: H95Q (32 nM), H95D (40 nM), Y96C (39 nM), Y96D (20 nM) and R68S (22 nM), compared with greater than 1μM for MRTX849. Furthermore, with the SW480 (G12V) in vivo xenograft model, TEB-17231 showed clear tumor growth inhibition with QD dosing for 4-8 mg/kg PO without body weight loss. These properties highlight TEB-17231 as a potential clinically actionable inhibitor for the KRAS-modified tumor population and warrant investigation of TEB-17231 in combination with other agents in the future."

Oncology • HRAS • KRAS • NRAS

"#280Bio Provides Update on the #KRASInhibitor #TEB17231 at the #AACR23 https://t.co/tIS3eL0SLi" (@1stOncology)

Oncology • KRAS

280Bio Provides Update on the KRAS Inhibitor TEB-17231 at the 2023 AACR Annual Meeting (PRNewswire) - "280Bio, Inc...announced a presentation featuring the Company's lead development candidate TEB-17231 at the AACR Annual Meeting in Orlando, Florida to be held April 14-19, 2023....The presentation describes preclinical findings on a lead series of small molecule inhibitors directed against multiple KRAS-mutation-altered tumor cell lines. The lead candidate TEB-17231 showed robust tumor growth inhibition, against KRASG12V, KRASG12C, KRASG12D and other RAS mutant tumor cell lines. TEB-17231 was also shown to be active in blocking tumor growth in KRASG12C-resistant cell lines bearing different secondary mutations in KRAS. With its excellent pharmacologic properties, TEB-17231 oral dosing demonstrates strong inhibition of in vivo KRAS mutant xenograft tumor growth."

Preclinical • Oncology