OBI Pharma Announces Acquisition of the Novel First-in-class Anti-Cancer Drug OBI-3424 from Threshold Pharmaceuticals to be Developed as Potential Anti-Cancer Therapy for Cancers with High AKR1C3

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April 26, 2017
Supplemental information on the approved application of Phase III clinical trial of OBI-822, the novel breast cancer drug, in China, US, and the EU
June 11, 2017
  1. Date of occurrence: June 01, 2017
  2. Company name: OBI Pharma, Inc.
  3. Relationship to the Company (please enter ”head office” or ”affiliated company”): N/A
  4. Reciprocal shareholding ratios: N/A
  5. Name of mass media: China Times E-Paper
  6. Content reported: OBI Pharma (4174) announced the in-licensing of the novel first-in-class small molecule drug TH-3424 from California Threshold Pharmaceuticals. The contract includes the global intellectual property rights and patent rights (excluding China, Hong Kong, Macau, Taiwan, Japan, Korea, Singapore, Malaysia, Thailand, Turkey, and India). The drug, renamed to OBI-3424, will be developed as a potential aldo-keto reductase 1c3 (AKR1C3) targeted anti-cancer therapy for cancers with high AKR1C3 expression. It will become one of the newest forces on OBI’s product line.
  7. The reason for this: OBI Pharma, Inc. announced today an agreement with Threshold Pharmaceuticals, Inc. to acquire TH-3424, a first-in-class novel small-molecule prodrug, renamed to OBI-3424. The drug will become one of the newest forces on OBI’s product line.
    OBI-3424 is designed to use the cancer-expressed AKR1C3 enzyme to activate the prodrug to selectively release DNA alkylating agent, a potent anti-cancer molecule. This kind of selective activation mechanism has great differences from the conventional alkylating agents, such as cyclophosphamide and ifosfamide.
    AKR1C3 overexpression has been documented in a number of treatment-resistant and difficult-to-treat cancers. For example, hepatocellular carcinomas (HCC), which highly overexpress AKR1C3 in most patients. OBI-3424 has demonstrated potent activities in preclinical models of HCC, including a model resistant to the standard of care treatment, sorafenib. AKR1C3 is adaptively upregulated in response to castration; therefore, castrate-resistant prostate cancer is another logical unmet need population where OBI-3424 will be tested. In addition, the US National Cancer Institute is performing preclinical evaluations of OBI-3424 for the potential treatment of T-cell acute lymphoblastic leukemia (T-ALL).
    Furthermore, individualized patient selection by staining for AKR1C3 overexpression by immunohistochemistry can be performed to identify patients with other tumor types most likely to respond to treatment with OBI-3424, thereby offering the possibility for a streamlined clinical development strategy.
    Under the terms of the agreement, Threshold will transfer to OBI Pharma its ownership rights as well as preclinical and manufacturing data for OBI-3424 in exchange for an undisclosed, upfront one-time payment. No further payments or future royalties are required. OBI Pharma will obtain Threshold’s global intellectual property as well as the commercial, developmental, and manufacturing rights to OBI-3424, except in certain specified countries in Asia (see footnote 1).
    Footnote 1: OBI Pharma owns Global intellectual property rights and patent rights, excluding the following countries: China, Hong Kong, Macau, Taiwan, Japan, Korea, Singapore, Malaysia, Thailand, Turkey, and India.
  8. Countermeasures: N/A.
  9. Any other matters that need to be specified: N/A.