Innovent and Laekna Jointly Announce First Patient Dosed with Three-drug Combination in a Phase 1/2 Study for the Treatment of Patients with Solid Tumors Who Were Resistant to Prior Anti-PD-1/PD-L1 Therapy

On July 31, 2022 Innovent Biologics, Inc. ("Innovent") (HKEX: 01801), a world-class biopharmaceutical company that develops, manufactures and commercializes high-quality medicines for the treatment of cancer, autoimmune, metabolic, ophthalmology and other major diseases, and Laekna Therapeutics, a clinical-stage biotechnology company dedicated to bringing ground-breaking therapies to cancer and liver fibrosis patients worldwide, reported that the first patient has been dosed in a Phase 1/2 clinical trial (clinicaltrials.gov, NCT05383482) of a three-drug combination therapy (afuresertib + sintilimab + chemotherapy) in patients with specific solid tumors who were resistant to anti-PD-1/PD-L1 therapy at the West China Second Hospital of Sichuan University (Press release, Innovent Biologics, JUL 31, 2022, View Source [SID1234617158]). This marks a key milestone on the first anniversary of the clinical research partnership established between Innovent and Laekna in July 2021.

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The study is a multi-center, single-arm, open-label, dose-escalation Phase 1/2 clinical study, assessing recommended Phase 2 dose (RP2D), safety, tolerability and anti-tumor activity of afuresertib in combination with sintilimab and chemotherapy (nab-paclitaxel or docetaxel) in patients with solid tumors who were resistant to prior anti-PD-1/PD-L1 therapy. The principal investigator of the study is Professor Lin Shen, Director of the Department of Gastrointestinal Oncology of Beijing Cancer Hospital. The primary endpoints of the Phase 1 dose escalation study are maximum tolerated dose (MTD) and RP2D, and the primary endpoint of the Phase 2 study is overall response rate (ORR). The study is planned to be extended as a multi-regional clinical trial at the pivotal stage.

The clinical trial assesses five types of solid tumors, including non-small cell lung cancer (NSCLC), gastric cancer/gastroesophageal junction cancer (GC/GEJC), esophageal cancer (EsC), cervical cancer (CC) and endometrial cancer (EC). The study focuses on the AKT inhibitor, a potential new therapy for drug resistant-cancer, to address the unmet medical needs in cancer immunotherapy resistance and bring hope to solid tumor patients who have received prior anti-PD-1/PD-L1 treatments.

The combination therapy consists of Laekna’s afuresertib (LAE002), a highly selective ATP competitive AKT inhibitor in pivotal clinical trials with favorable clinical efficacy and safety profile, and Innovent’s PD-1 inhibitor sintilimab (TYVYT), which has been approved for six indications in China with the first four included in the National Reimbursement Drug List (NRDL).

The subject who received the first dose was a patient with cervical cancer. Professor Rutie Yin, investigator of the center where the first patient was dosed and Director of the Department of Chemoradiotherapy Oncology at the West China Second Hospital of Sichuan University, said, "Cervical cancer is the fourth most common cancer globally in women1. In 2020, China reported about 110,000 new cases and about 60,000 death cases of cervical cancer2. Patients are faced with limited treatment options and the prognosis is poor3,4. Immunotherapy plays an increasingly important role in the treatment of recurrent or metastatic cervical cancer, and there is huge unmet need. With the launch of new immunosuppressants, they’ve been applied to more patients and become essential for the treatment of cervical cancer. AKT inhibitor, a serine/threonine-specific protein kinase, is considered a potential new target for cancer treatment as results of multiple preclinical studies showed that inhibition of AKT could restore the sensitivity of cancer cells to anti-tumor therapies. We look forward to the progress of the clinical trial and hope it will bring new breakthroughs to the later-line treatment of cervical cancer in China."

Professor Lin Shen, principal investigator of the study, Director of the Department of Gastrointestinal Oncology of from Beijing Cancer Hospital, stated, "Innovation never stops in oncology as we are always looking for new ways to treat cancer patients. Based on results from the preclinical and clinical studies, the combination of an immune checkpoint inhibitor, an AKT inhibitor and taxanes shows potential to be a new treatment option for patients who were resistant to immune checkpoint inhibitors5,6,7,8. The trial conducted by Laekna and Innovent aims to explore this innovative combination therapy and validate this new promising solution. There is a significant clinical need for patients with digestive system and gynecologic solid tumors in China; we hope to see that AKT-targeting therapy will prove to be an effective strategy to overcome drug resistance."

Dr. Hui Zhou, Senior Vice President of Innovent, stated, "With the increasing prescription of immune checkpoint inhibitors (ICI) in first-line settings in various tumor types, many patients developed ICI resistance or have poor response rates in clinical practice. It is of great clinical value to explore potential treatments for this huge unmet medical need. Sintilimab is the first PD-1 inhibitor in China with first-line indications for 5 major types of cancers. Innovent hopes to continue to develop the potential of high-quality drugs, in this case by combination therapy with Laekna’s innovative AKT inhibitor. We look forward to the results of clinical trial to bring clinical benefits to patients with specific solid tumors."

Dr. Yong Yue, Chief Medical Officer of Laekna, said, "It took less than six months to complete the journey from IND approval to dosing of first patient, showing robust strategic execution of Laekna’s global clinical team. There are three main considerations in selecting the five types of solid tumors: PD-1/PD-L1 inhibitors have been approved as the standard-of-care treatments for those cancers in multiple countries; higher rates of biomarkers that activate the AKT pathway in patients with resistance to anti-PD-1/PD-L1 therapy were observed in those cancers; and the incidence rates and death rates are relatively high in China. We hope this innovative three-drug combination therapy will benefit patients with these solid tumors."

About Afuresertib (LAE002)

Afuresertib (LAE002) is an investigational highly selective adenosine triphosphate (ATP) competitive AKT inhibitor.

Laekna in-licensed afuresertib from Novartis in 2018 and are conducting five combination therapy clinical trials for the treatment of ovarian cancer, prostate cancer, breast cancer, and PD-1/PD-L1-resistant solid tumors. Prior to Laekna’s in-licensing agreement, over 10 clinical trials had been conducted to demonstrate the safety and efficacy profiles of afuresertib. In the Phase Ib study conducted by Novartis, afuresertib showed potential anti-tumor efficacy in platinum-resistant ovarian cancer (PROC) patients with an overall response rate (ORR) of 32.1% and progression-free survival (PFS) of 7.1 months9. In pre-clinical studies, afuresertib has demonstrated its ability to restore platinum/paclitaxel sensitivity in PROC cell lines. After the in-licensing agreement, Laekna also identified the therapeutic potential of combining afuresertib and LAE001 (an investigational potential first-in-class next-generation androgen synthesis inhibitor that simultaneously inhibits both CYP17A1 and CYP11B2) and observed their synergistic anti-tumor efficacy in our completed Phase 1 and ongoing Phase 2 studies in metastatic castration-resistant prostate cancer (mCRPC) patients as second- to fourth-line treatments. According to Frost & Sullivan, afuresertib is one of the three AKT inhibitors worldwide that have entered pivotal clinical trials10.

About Sintilimab

Sintilimab, marketed as TYVYT (sintilimab injection) in China, is a PD-1 immunoglobulin G4 monoclonal antibody jointly developed by Innovent and Eli Lilly and Company. Sintilimab is a type of immunoglobulin G4 monoclonal antibody, which binds to PD-1 molecules on the surface of T-cells, blocks the PD-1 / PD-Ligand 1 (PD-L1) pathway, and reactivates T-cells to kill cancer cells11. Innovent is currently conducting more than 20 clinical studies of sintilimab to evaluate its safety and efficacy in a wide variety of cancer indications, including more than 10 registrational or pivotal clinical trials.

In China, sintilimab has been approved for six indications as below, with the first four included in the National Reimbursement Drug List (NRDL), including:

The treatment of relapsed or refractory classic Hodgkin’s lymphoma after two lines or later of systemic chemotherapy;
In combination with pemetrexed and platinum chemotherapy, for the first-line treatment of non-squamous non-small cell lung cancer lacking EGFR or ALK driver mutations;
In combination with gemcitabine and platinum chemotherapy, for the first-line treatment of squamous non-small cell lung cancer;
In combination with BYVASDA (bevacizumab biosimilar injection) for the first-line treatment of unresectable or advanced hepatocellular carcinoma;
In combination with cisplatin plus paclitaxel or cisplatin plus 5-fluorouracil for the first-line treatment of esophageal squamous cell carcinoma;
In combination with fluorouracil and platinum-based chemotherapy for the first-line treatment of unresectable, locally advanced, recurrent or metastatic gastric or gastroesophageal junction adenocarcinoma.
Innovent currently has the regulatory submission for sintilimab in combination with bevacizumab biosimilar and chemotherapy for EGFR-mutated non-squamous NSCLC following EGFR-TKI treatment under review in the China’s NMPA.

Additionally, two clinical studies of sintilimab have met their primary endpoints:

Phase 2 study as second-line treatment of esophageal squamous cell carcinoma;
Phase 3 study as second-line treatment for squamous NSCLC with disease progression following platinum-based chemotherapy.