Shanghai, China and New Jersey, U.S., September 16, 2021 - Laekna Therapeutics, an emerging innovative biotech company based in China’s “Zhangjiang Pharma Valley” and New Jersey, USA, focusing on the development of ground-breaking innovative therapies to treat cancer and liver diseases, reported positive results in two clinical studies for the treatment of early and late stages of prostate cancer respectively at the European Society for Medical Oncology (ESMO) Congress 2021 today.

The first study with LAE001 monotherapy targeting early stage of prostate cancer, and the second study with combination therapy of LAE001 + afuresertib in drug-resistant late stage prostate cancer, demonstrated positive and encouraging results by Laekna Therapeutics.

E-Poster:597P

A Phase I Dose-Escalation Study of LAE001 In Patients with Metastatic Castration-Resistant Prostate Cancer (mCRPC)

Lead author and presenter: Dr. Dingwei Ye (Shanghai, China)

This ClinicalTrials NCT03843918 is a phase I dose-escalation and expansion study of LAE001 monotherapy without steroid, in patients with metastatic castration-resistant prostate cancer (mCRPC). LAE001 is the first CYP17A1/CYP11B2 dual inhibitor globally.

Results:

As of May 25, 2021, 27 pts (16, 5, 3, 3 pts in the 50, 75, 100 and 125 mg BID cohorts, respectively) enrolled in the phase Ia & Ib part and had a median 7.3 months follow up (1-25 months). Based on safety data, 50mg BID of LAE001 was selected as the RP2D; no DLT nor AE leading to discontinuation was reported under the RP2D, and the related serious adverse event (SAE) in the RP2D cohort was 6%.

 Out of 15 patients treated in 50mg bid cohort, 11 pts (73%) had a >50% best PSA decline from baseline, among whom 6 pts (40%) had >90% PSA decline from baseline.

2 pts (50mg bid) had a PSA response that sustained for >52 weeks; 81% patients are ongoing treatment at the cut-off date.

Conclusions:

LAE001 monotherapy without steroid co-use is safe and well-tolerated at 50mg BID level (RP2D). The preliminary antitumor activity of LAE001 monotherapy at RP2D level supports the potential clinical benefit of treating patients with mCRPC. Further expansion phase 1b and II [1]study at RP2D is ongoing.

E-Poster: 599P

A Phase I Dose-Escalation Study of LAE001/Prednisone Plus Afuresertib in Patients with Metastatic Castration-Resistant Prostate Cancer (mCRPC) Following Standard of Care (SOC) Treatment

Lead author and presenter: Dr. Alberto Bessudo (Encinitas, CA, United States of America)

This ClinicalTrials NCT04060394 is a phase I dose-escalation study of a combination therapy with LAE001/prednisone plus afuresertib in patients with metastatic castration-resistant prostate cancer (mCRPC) following failed average 3,3 lines of prior SOC treatments. Afuresertib (LAE002) is an oral, small molecule pan-AKT kinase inhibitor. Whereas LAE001 is the first CYP17/CYP11B2 dual inhibitor globally.

Results:

As of 06/29/2021, 14 pts (8 in cohort 1 and 6 in cohort 2) received study treatment with median 12.5 months follow up. The dose of LAE001 75 mg BID/prednisone 5 mg BID and afuresertib 125 mg QD was determined as the RP2D. 2 DLTs were reported in cohort 1 (thrombocytopenia) and cohort 2 (skin rash), respectively, and only one non-DLT grade >= 3 treatment-emergent adverse events (TEAE) (skin rash) in cohort 2 (RP2D).

2 pts had a PSA response (2/10, 20%). Among 5 pts who have measurable lesions, 1 PR and 2 SDs were reported.

The 10 evaluable pts on average had failed 3.3 lines of SOC.

Conclusions:

The combination therapy of LAE001 75mg BID/prednisone 5mg BID and afuresertib 125mg QD was determined as the RP2D. The preliminary antitumor activity under the RP2D supports the potential clinical benefit for treating drug-resistant mCRPC and moves forward this study to phase II stage.

Encouraging results for patients with prostate cancer to soon benefit from LAE001 and afuresertib

“As an emerging innovative biotech company, Laekna Therapeutics is proud to make its debut at the ESMO Congress. We are very pleased to present the results from two clinical studies at this influential academic conference,” said Dr Yue Yong, Chief Medical Officer of Laekna Therapeutics.

Prostate cancer is the most common cancer occurring in men world-wide. The monotherapy trial of LAE001 showed that the drug can be used without prednisone, and still demonstrate a tolerable safety profile and strong anticancer efficacy. Laekna plans to further develop LAE001 for patients with mHSPC who require a much longer treatment duration, and would benefit more from the ability to use LAE001 without prednisone.

Currently there is limited treatment options for NAAR drug-resistant mCRPC patients. The combination therapy of LAE001 and afuresertib is intended to benefit patients with PTEN/PIK3CA/AKT alterations.

“The topline data reported by Laekna Therapeutics at the ESMO Congress, a top international academic conference marks significant progress for Laekna’s clinical programs,” Dr Yue Yong remarked. “With the continued advancement of the above two studies, we have seen more encouraging results in the enrolled patients in the past three months. We hope patients with both early- and late-stage prostate cancer can soon benefit from these two new innovative medicines.”

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About European Society for Medical Oncology (ESMO) Congress 2021

The ESMO Congress is one of the most influential oncology forums, where participants present the latest advances in the treatment of cancer and have cross-discipline exchanges and discussions. In response to the COVID-19 pandemic, the congress will be held virtually September 16-21, 2021.

About CYP17A1/CYP11B2 dual inhibitor (LAE001)

LAE001 is the first CYP17/CYP11B2 dual inhibitor globally. It is a novel, potent, non-steroidal, reversible dual inhibitor of CYP17 and CYP11B2 (aldosterone synthase) that blocks both androgen and aldosterone synthesis. It will be used as a treatment option for metastatic prostate cancer.

Compared to Abiraterone acetate, a CYP17 enzyme inhibitor that causes hyperaldosteronism, which requires long-term use of corticosteroids and may cause serious side effects, LAE001 has demonstrated similar therapeutic efficacy and improved safety profile in patients with drug-resistant mCRPC. Due to its dual inhibition of both CYP17 and CYP11B2, two critical enzymes for testosterone and aldosterone synthesis, LAE001 does not increase aldosterone level, therefore reduces the risk of cardiovascular toxicity and hepatotoxicity related to long-term prednisone use.

About Afuresertib（LAE002）

Afuresertib (LAE002) is a differentiated oral, small molecule pan-AKT kinase inhibitor that has been investigated in over 10 Phase 1/2 clinical trials, including ovarian cancer, gastric cancer, multiple myeloma, and melanoma. These studies have demonstrated that afuresertib has strong anti-cancer activities and a tolerable safety profile. The global randomized, open-label, multi-center Phase 2 PROFECTA-II clinical trial of afuresertib is the world’s first registration-directed clinical study of a pan-AKT kinase inhibitor to treat platinum-resistant ovarian cancer.

In recent years, AKT (a serine/threonine-protein kinase) has emerged as an important mechanism in oncology, as it plays an important role in regulating various cell functions such as metabolism, survival, proliferation, tissue invasion, and chemotherapy resistance. PTEN deletion and AKT/PIK3CA alteration may lead to excessive activation of the AKT signaling pathways, which is one of the key drivers for cancer growth. The increased activation of the AKT signaling pathway is particularly common in recurrent ovarian cancer, breast cancer, and prostate cancer.

About Laekna Therapeutics

Founded in December 2016, Laekna Therapeutics is an emerging innovative pharma company based in China’s “Zhangjiang Pharma Valley” and New Jersey in the US, focusing on developing new ground-breaking innovative therapies to treat cancer and liver diseases.

Laekna Therapeutics has adopted a two-pronged strategy in new drug development. On one hand, it continues to enrich its portfolio by introducing global new drugs with the clinical Proof of Concept. The company has obtained the global exclusive rights of four new drug candidates from Novartis. On the other hand, the company’s self-developed innovative drugs will soon enter clinical development stage.

Laekna has set up a team of top global pharmaceutical talent. Its leadership team members each have over 20 years of experience in new drug development in China and the US, with an exceptional track record in R&D, new drug approvals and commercialization. Laekna is committed to a science-based, innovation-driven approach to create an international leading clinical research and development platform for the development of first-in-class and best-in-class innovative drugs.

The detailed Laekna Therapeutics information can be found from the website: http://www.laeknatp.com

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