WXFL10030390 / Guangzhou JOYO Pharma - LARVOL DELTA

In Vivo PK-PD and Drug-Drug Interaction Study of Dorzagliatin for the Management of PI3Kα Inhibitor-Induced Hyperglycemia. (PubMed, Pharmaceuticals (Basel)) - "Objectives: The anticancer effects of PI3Kα inhibitors (PI3Ki) are constrained by their hyperglycemic side effects, while the efficacy of conventional hypoglycemic agents, such as insulin, metformin, and SGLT-2 inhibitors, in mitigating PI3Ki-induced hyperglycemia remains suboptimal. Our findings indicate that the drug-drug interactions (DDIs) between dorzagliatin and multiple PI3Ki (including WX390 and BYL719) may partially account for the enhanced antitumor efficacy observed in the combination therapy group compared to PI3Ki monotherapy. This interaction may be explained by the inhibition of P-glycoprotein (P-gp) and the pharmacological mechanism of dorzagliatin regarding the activation of insulin regulation."

Journal • PK/PD data • Preclinical • Diabetes • Oncology • PIK3CA

PIK3CA inhibitor treatment for metastatic scrotal extramammary Paget's disease: a case report and literature review. (PubMed, AME Case Rep) - "The treatment response was evaluated as stable disease (SD) after 6 courses of docetaxel plus tegafur (DS regimen) chemotherapy. Then, a second-line treatment, a PIK3CA inhibitor, WX390, was administered with tolerable toxicity...To the best of our knowledge, this is the first case report of a PIK3CA inhibitor for the treatment of primary metastatic EMPD, and the treatment efficacy was good. PIK3CA inhibitors may be promising for the treatment of metastatic EMPD in the future."

Journal • Oncology • Rare Diseases • PIK3CA

Preliminary outcomes from a phase 1b/2 study of the highly potent PI3K-mTOR dual inhibitor WX390 combined with toripalimab in patients with advanced cervical cancer (AACR 2025) - P1/2 | "WX390 in combination with Toripalimab had a manageable safety profile and promising efficacy in patients with advanced cervical cancer, including encouraging antitumor effects in CPI-pretreated patients."

Clinical • IO biomarker • Metastases • P1/2 data • Cervical Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma • PIK3CA • PIK3CD • PIK3CG

The latest clinical study results of Jiayue Pharmaceutical’s JYP0322 and WX390 were selected for AACR 2025 [Google translation] (bydrug.pharmcube.com) - "From April 25 to 30, 2025, the 2025 Annual Meeting of the American Association for Cancer Research (AACR) will be held in Chicago, USA. Jiayue Pharmaceutical will present the latest Phase I clinical study results of the new generation ROS1 inhibitor JYP0322 in patients with ROS1 gene fusion-positive advanced non-small cell lung cancer (NSCLC) in the form of an oral report. This is the first data publication of JYP0322 in NSCLC patients. In addition, the company will also present the latest clinical research results of the innovative drug WX390 (PI3K/mTOR dual-target inhibitor) combined with toripalimab in the treatment of patients with advanced cervical cancer through posters."

P1 data • P1/2 data • Cervical Cancer • Non Small Cell Lung Cancer • Solid Tumor

Targeting on the PI3K/mTOR: a potential treatment strategy for clear cell ovarian carcinoma. (PubMed, Cancer Chemother Pharmacol) - "This study comprehensively assessed the efficacy of WX390 across multiple models of OCCC, laying a solid foundation for the development of new therapeutic strategies for this challenging malignancy."

Journal • Clear Cell Carcinoma • Gynecologic Cancers • Oncology • Ovarian Cancer • Ovarian Clear Cell Cancer • Solid Tumor

A Study of WX390 Combined With Toripalimab in Patients With Advanced Gastric-type Endocervical Adenocarcinoma With STK11 Mutations (clinicaltrials.gov) - P2 | N=20 | Recruiting | Sponsor: Shanghai Jiatan Pharmatech Co., Ltd | Trial completion date: Dec 2025 ➔ Dec 2026

Metastases • Trial completion date • Cervical Cancer • Gastric Cancer • Oncology

JYP0390M203: A Study of WX390 Combined With Toripalimab in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1/2 | N=100 | Recruiting | Sponsor: Shanghai Jiatan Pharmatech Co., Ltd | Trial completion date: Mar 2025 ➔ Nov 2025 | Trial primary completion date: Mar 2025 ➔ Nov 2025

Metastases • Trial completion date • Trial primary completion date • Oncology • Solid Tumor

WX390-002: A Study of WX390 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P2 | N=70 | Recruiting | Sponsor: Shanghai Jiatan Pharmatech Co., Ltd | Trial completion date: Jun 2024 ➔ Jun 2026 | Trial primary completion date: Jun 2024 ➔ Jun 2025

Metastases • Trial completion date • Trial primary completion date • Oncology • Solid Tumor

Preliminary outcomes from a phase Ib/II study of the highly potent PI3K-mTOR dual inhibitor WX390 combined with toripalimab in patients with advanced cervical cancer (ESMO 2024) - P1/2 | "WX390 combined with Toripalimab demonstrated a manageable safety profile and promising antitumor effects in patients with advanced cervical cancer. Further assessments of antitumor response and safety are currently ongoing in a larger cohort of patients."

Clinical • Metastases • P1/2 data • Cervical Cancer • Head and Neck Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma of Head and Neck • Urothelial Cancer

Preliminary outcomes from a phase Ib/II study of WX390 combined with toripalimab in patients with recurrent or metastatic head and neck squamous cell carcinoma (ESMO 2024) - P1/2 | "WX390 combined with Toripalimab demonstrated a manageable safety profile and encouraging antitumor effects in patients with R/M HNSCC. Further evaluations of this combination are ongoing."

Clinical • Metastases • P1/2 data • Cervical Cancer • Head and Neck Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Carcinoma of Head and Neck • Urothelial Cancer

Translational study and preliminary clinical trial of WX390 monotherapy in cancers with concurrence of PIK3CA and ARID1A mutations (ESMO 2024) - P2 | "Co-occurring PIK3CAmut- ARID1Amut is highly prevalent in human cancers and may indicate enhanced response to WX390. WX390 had a manageable safety profile and encouraging efficacy in platinum resistant OCCC pts, especially for the PIK3CAmut- ARID1Amut sub-group. Further evaluation of efficacy and safety are ongoing."

Clinical • Monotherapy • Gynecologic Cancers • Oncology • Ovarian Cancer • ARID1A • PIK3CA

PIK3CA mutations enhance the adipogenesis of ADSCs in facial infiltrating lipomatosis through TRPV1. (PubMed, iScience) - "Our study showed that PIK3CA mutations promoted adipogenesis in FIL-ADSCs and this effect was achieved by suppressing TPRV1. Pathogenesis experiments suggested that WX390 may serve as an agent for the treatment of FIL."

Journal • Metabolic Disorders • PIK3CA • TRPV1

Phase Ib study of a high potent PI3K-mTOR dual inhibitor WX390 combined with toripalimab in patients with advanced solid tumors. (ASCO 2024) - P1/2 | "WX390 in combination with Toripalimab had a manageable safety profile and encouraging antitumor effects in patients with advanced solid tumors. An RP2D of 1. 1 mg qd of WX390 in combination was selected to be explored in further phase II study, which is ongoing in different tumor types."

Clinical • Metastases • P1 data • Cardiovascular • Cervical Cancer • Dental Disorders • Diabetes • Fatigue • Genito-urinary Cancer • Head and Neck Cancer • Heart Failure • Hematological Disorders • Leukopenia • Oncology • Renal Disease • Solid Tumor • Stomatitis • Thrombocytopenia • Urothelial Cancer

A Study of WX390 in Patients With Advanced Solid Tumors With PIK3CA Mutations (clinicaltrials.gov) - P1/2 | N=38 | Completed | Sponsor: Shanghai Jiatan Pharmatech Co., Ltd

Metastases • New P1/2 trial • Oncology • Solid Tumor • PIK3CA

A Study of WX390 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P2 | N=70 | Recruiting | Sponsor: Shanghai Jiatan Pharmatech Co., Ltd

Metastases • New P2 trial • Oncology • Solid Tumor

A Study of WX390 Combined With Toripalimab in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1/2 | N=100 | Recruiting | Sponsor: Shanghai Jiatan Pharmatech Co., Ltd

Metastases • New P1/2 trial • Oncology • Solid Tumor

A Study of WX390 Combined With Toripalimab in Patients With Advanced Gastric-type Endocervical Adenocarcinoma With STK11 Mutations (clinicaltrials.gov) - P2 | N=20 | Recruiting | Sponsor: Shanghai Jiatan Pharmatech Co., Ltd

Metastases • New P2 trial • Cervical Cancer • Gastric Cancer • Oncology

A Study of WXFL10030390 in Patients With Advanced Solid Tumors or Lymphoma (clinicaltrials.gov) - P1 | N=82 | Completed | Sponsor: Shanghai Jiatan Pharmatech Co., Ltd | Unknown status ➔ Completed | N=42 ➔ 82

Enrollment change • Metastases • Trial completion • Hematological Malignancies • Lymphoma • Oncology • Solid Tumor

[VIRTUAL] WX390, a high-potent PI3K-mTOR dual inhibitor, first-in-human (FIH) phase I study in advanced relapsed or refractory solid tumor, and lymphoma. (ASCO 2021) - P1 | "the PI3K-mTOR dual inhibitor WX390 was well tolerated with manageable safety profile, and showed encouraging antitumor activity . A RP2D of 1.1 mg qd is selected to be explored for different indications in solid tumor clinical studies."

P1 data • Anemia • Cervical Cancer • Dermatitis • Dermatology • Diabetes • Follicular Lymphoma • Head and Neck Cancer • Hematological Disorders • Hematological Malignancies • Immunology • Lymphoma • Metabolic Disorders • Neutropenia • Oncology • Solid Tumor • Thrombocytopenia • PIK3CA