Green Chemistry Platform for Targeted Drug Delivery and R&D
Empiriko’s proprietary Green Chemistry platform includes a series of azamacrocycles, biological enzymes/processes and AI/computational modeling.
Key Features of Novel Azamacrocycles
Empiriko’s synthetically modified azamacrocycles mimic the functionalities of the organic building blocks which naturally occur in human and other species (i.e., hemoglobin, cytochrome P450). These azamacrocycles are complexed with various metals to make proprietary oxidants with targeted functionalities which can be used in medicinal chemistry, environmental health, clean energy, and other areas of the life sciences. The company has successfully synthesized and reproducibly scaled compounds that are stable in a variety of aqueous systems.
Key functions
Biomimetic: Empiriko has developed an animal free proprietary in vitro chemosynthetic liver technology (Biomimiks™) that closely mirrors the in vivo metabolism of hepatic enzymes (cytochrome P450), providing an effective platform to identify and quantitate reactive, toxic, and unstable metabolites for small molecule drug discovery and development.
Metal Incorporation: Empiriko’s proprietary technology can incorporate radioactive nuclides into water soluble azamacrocycles (radioactive carrier vehicle complex=RCV™) which enable targeted delivery of a focused radioactive payload to tumors at the cellular level. Clinically this reduces toxicity, damage to healthy tissues and shortens treatment duration. RCV™s can be used as “theranostics” for both therapeutic intervention and diagnostic radiotracing at the cellular level.
Oxidative degradation: As drug delivery carriers, azamacrocycles also function as a codrug which amplifies radioligand and antibody drug conjugate (ADC) efficacy, lowers doses and shortens treatments. These ADCs also can be applied as targeted treatments for conditions beyond oncology.
Opportunities
Beyond drug discovery and development, Empiriko’s Green Chemistry platform creates a range of opportunities in several industries to address some of society’s most pressing problems at the intersection of the life sciences, environmental health, food safety, water remediation (AquaRemediate™) and the production of biofuels (ChemBiofuels™). The company is actively exploring opportunities to apply its technology in these burgeoning fields.
Radioligand Therapy
Radioligand therapy (RLT) represents a paradigm shift in cancer treatment and disease monitoring and is one of the fastest growing markets within the pharmaceutical industry. This promising advancement in precision oncology delivers targeted radiation to cancer cells at the cellular level. By combining antibodies with a therapeutic radionuclide, RLT immunologically targets cancer cells expressing specific biomarkers to precisely deliver cytotoxic radiation.
Empiriko’s Radioligand Enhanced Cancer Treatment via Linker-Antibody Immunotherapy Macrocycles (R*ECL-AI-M™) platform
Empiriko’s R*ECL-AI-M™ platform includes proprietary radioactive azamacrocycles, linkers and tumor specific antibodies. Radioactive azamacrocycles are covalently linked to tumor specific antibodies which once in circulation, bind to tumor specific antigens. Conjugates bind/enter/kill cancer cells or other targets by delivering focused radiation / nascent oxygen at the cellular level. Azamacrocycles can be complexed with radioactive isotopes that are alpha, beta and auger electron particle emitters with distinctive characteristics in strength and penetrating distance.
As a drug delivery carrier, azamacrocycles can function as a codrug which amplifies both radioligand and antibody drug conjugate (ADC) efficacy, lowers doses and shortens treatments. R*ECL-AI-M™’s distinctive properties, efficacy, and limited toxicity profile can be leveraged to create a theranostic platform to treat primary and metastatic tumor burdens across a range of clinically relevant scenarios.
EMP 108: Targeted Radioligand Therapy for Prostate Cancer
Empiriko’s EMP108 is a targeted radioligand therapy for prostate cancer consisting of a tumor specific antibody which binds to a prostate-specific membrane antigen (PMSA) target, ¹⁷⁷Lu radiometal and RCV™ carrier. After antigen-antibody binding takes place, EMP108 enters the prostate cancer cell via endocytosis and delivers beta radiation which damages DNA inside the cancer cell. In addition, the RCV™ carrier for EMP108 irreversibly damages DNA and cellular organelles via singlet oxygen radicals leading to cell death. At the clinical level, these synergies translate into shorter treatment duration, lower drug doses and fewer side effects.
EMP 116: Novel Radio + Chemo Dual Therapy for Prostate Cancer
Empiriko’s EMP 116 delivers a targeted simultaneous bilateral delivery of chemotherapy and radiation to prostate tumors. EMP116 drug consists of a tumor specific antibody which binds to a PSMA target, ¹⁷⁷Lu radiometal and it attaches a selectively modified RCV™ to a specific chemo drug to form an RCV™-Chemo-Ab complex. The newly formed RCV™ -Chemo-Ab complex delivers chemotherapy and radiation
in a site-specific manner at the cellular level. This chemical flexibility creates a new scalable platform which can simultaneously deliver an array of Radio+ChemoRx NCEs to cellular targets anywhere in the body based on antibody specificity, limiting side effects to adjacent healthy tissues.
EMP 102-Dx: Radiotracer for Prostate Cancer
Empiriko’s radioligand EMP102-Dx radiotracer consists of a tumor specific antibody which binds to a PSMA target, ⁶⁸Ga radiometal and RCV™ carrier. After the antigen-antibody interaction takes place, EMP102-Dx enters the prostate cancer cell via endocytosis. Subsequently, ⁶⁸Ga emits beta radiation which is detected by PET/CT scan. PET/CT scans with EMP102-Dx radiotracers detect cancer cells, monitors tumor progression/metastases and response to treatment.
Advancing Precision Medicine and
Personalized Cancer Treatment
The promise of “Precision Medicine” where patient-specific, targeted therapies overcome the challenges of individual variability is one of the most rapidly evolving areas of healthcare. Novel approaches which leverage advanced modalities like radiopharmaceuticals and antibody-drug conjugates (ADCs) are now a reality and will extend the possibilities for patient-specific care in the near future.
Empiriko’s innovative portfolio and immuno-chemo-radio drug pipeline has the potential to redefine drug development and improve patient outcomes. Combining these patient-specific targeted therapies with patient monitoring (via Empiriko’s PMF™ device) will provide a suite of services to treat diseases, monitor outcomes, and provide personalized care.
Pipeline
Empiriko’s scalable platform can embed multiple radioactive nuclides and antibody drug conjugates, to rapidly generate new chemotherapeutic agents. Empiriko’s current drug pipeline focuses on prostate, GEP-NET and ovarian cancers. Empiriko’s pipeline includes radioligand therapy, radio+chemo dual therapy, as well as ADCs and radiotracers across multiple assets in the pipeline.
