KPS Introduces FRα Anticancer Drug Metabolite... "Targeting 8 Trillion Won Ovarian Cancer Market"

KPS announced on the 12th that its bio-subsidiary Algok Bio has signed an exclusive global development and commercialization agreement for the folate receptor alpha (FRα)-targeting small molecule drug candidate Idetrexed with BTG International, a subsidiary of the global biotech Boston Scientific.

The drug candidate Idetrexed selectively binds to the FRα receptor, which is known to be overexpressed in cancer cells, penetrates into the cells, and induces cancer cell death by inhibiting the activity of thymidylate synthase, an enzyme essential for DNA replication in cancer cells. This is its mechanism of action (MoA).

Idetrexed was led by ICR, BTG’s co-development partner, in a clinical trial conducted until 2019 involving 109 patients with platinum-resistant ovarian cancer (average age 62). Among 25 patients with FRα overexpression (medium or high) who received the maximum tolerated dose (MTD), an objective response rate (ORR) of 36% was recorded. These results were published last year in Clinical Cancer Research, a leading international journal of the American Association for Cancer Research (AACR).

In platinum-resistant ovarian cancer, which shows resistance to platinum-based chemotherapy, ORR is a highly important evaluation metric that can determine FDA approval, as there were no other treatment options and the ORR was only about 10-15%.

Notably, in November last year, ImmunoGen, a U.S. biotech company, received accelerated FDA approval for Elahere (generic name: Mirvetuximab Soravtansine), an antibody-drug conjugate (ADC) targeting FRα, for the indication of platinum-resistant ovarian cancer. Elahere, the only competing drug to Idetrexed, has an ORR of only 27.4% and is associated with side effects such as ocular toxicity and hematologic cell reduction.

Kim Seong-cheol, CEO of Algok Bio, stated, "Considering Elahere’s clinical results, Idetrexed can be recognized as best-in-class not only in clinical utility but also in safety. The side effects of the small molecule Idetrexed are mild, including gastrointestinal disorders, asthenia, and arthralgia."

Furthermore, Idetrexed’s potential as a drug includes the possibility of synergistic effects when combined with PARP inhibitors (Poly ADP-Ribose Polymerase Inhibitors), which are considered game changers in the anticancer drug market. Through combination clinical trials with PARP inhibitors, indications can be expanded to include platinum-sensitive ovarian cancer patients as well as breast cancer, prostate cancer, pancreatic cancer, and other existing PARP inhibitor treatment areas. Preclinical studies confirmed that Idetrexed increased efficacy more than 20-fold when combined with the PARP inhibitor Lynparza (generic name: Olaparib).

The accelerated approval of Elahere has also positively impacted the global anticancer market by rapidly increasing the value of FRα. Multinational pharmaceutical company Bristol-Myers Squibb (BMS) signed a contract worth up to $3.1 billion (approximately 3.515 trillion KRW) with Japanese pharmaceutical company Eisai for the co-development of the FRα ADC therapeutic 'MORAb-202.'

CEO Kim said, "In the still unmet medical needs area of platinum-resistant ovarian cancer, we plan to design a personalized treatment strategy for patients with FRα overexpression and enter late-stage Phase 2(b) clinical trials in the second half of the year. We aim to challenge the End-of-Phase 2 (EOP2) meeting to prepare for fast track designation and Phase 3 clinical trials by the end of 2025. At the same time, we will accelerate the development of combination therapies with PARP inhibitors, Avastin (generic name: Bevacizumab), and others to expand Idetrexed’s indications."

With this, Algok Bio has secured its second pipeline capable of late-stage clinical trials since December 2021, when it first introduced the global drug candidate AGK-102, an antibody anticancer agent targeting the cancer stem cell surface protein 'TM4SF4,' from the Korea Atomic Energy Research Institute. The company is dedicated to researching and developing innovative therapies using platform technology to address unmet medical needs.

Meanwhile, according to the GlobalData Report, more than 240,000 ovarian cancer patients are diagnosed annually, and the global ovarian cancer market is projected to reach $6.7 billion (approximately 8.5 trillion KRW) by 2028, with a compound annual growth rate (CAGR) of 14.4%. The PARP inhibitor anticancer drug market is expected to account for 41.8% of the total ovarian cancer market during the same period, primarily in platinum-sensitive ovarian cancer.