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The journey from molecule to medicine starts with understanding its path inside the body. DMPK (Drug Metabolism and Pharmacokinetics) plays a crucial role in early drug discovery helping answer key questions about a compound’s absorption, distribution, metabolism, and excretion. These insights are essential to optimise the pharmacokinetic and safety profile of lead candidates and to improve the likelihood of downstream success.
Bringing new therapies to patients demands speed, data quality, and decision-making. At o2h Discovery, we are passionate about accelerating ideas into medicines. We understand that early-stage drug discovery is driven by a delicate balance of chemistry, biology, and pharmacokinetics and we are here to help you get that balance right, faster.
Our integrated drug discovery (IDD) platform brings together world-class capabilities in synthetic chemistry, biology, and DMPK. To give you a closer look into our approach, this edition features a real-world case study highlighting what makes o2h’s DMPK offerings uniquely positioned to support diverse modalities.
Kind regards,
Prashant Shah
CEO, o2h Discovery
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DMPK Capabilities
At o2h Discovery, we offer a comprehensive suite of in-vitro ADME assays including microsomal/hepatocyte/s9 stability, plasma protein binding, CYP inhibition/induction, permeability (PAMPA/Caco-2), solubility, and plasma/blood stability, among others. These assays are conducted alongside our chemistry teams, enabling real-time coordination between teams, resulting in faster turnaround of data. This proximity and agility significantly compress the design-make-test cycle allowing for more iterative data-driven decisions during the lead optimisation phase.
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With two decades of proven experience supporting global discovery programs, our teams bring robust domain expertise to the table ready to deliver both targeted functional support and end-to-end discovery execution with speed and precision.
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Case Study: Integrated Solutions for Biotech Drug Development
Objective - To streamline and scale the hit-to-lead optimisation of a promising series, o2h Discovery brought together its multi-disciplinary expertise spanning medicinal chemistry, synthetic and process chemistry, biology, DMPK, and preclinical toxicology. Our integrated support included assay development, compound screening, SAR analysis, in vitro ADME profiling, and iterative lead optimisation including in-vivo PK and tox studies enabling data-driven decisions and seamless progression across the discovery and development pipeline.
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Medicinal Chemistry
- Supported the client with target design strategies and chemistry hypothesis generation based on preliminary screening outcomes.
- Regular reviews of SAR and ADME data enabled the design of new analogs to improve potency and pharmacokinetic properties.
- Integrated design-make-test cycles accelerated the identification and progression of a promising lead candidate.
Synthetic Chemistry
- The lead molecule was successfully synthesised at Kg scale, demonstrating scalability and process robustness.
- A mixture of diastereomers was synthesised, which was further separated by chiral separation to get a single diastereomer with >99% chiral purity at multi kg scale.
- Both synthesis and purification were executed in multiple batches to ensure consistency across scale-up.
Biology
- Developed and optimised high-throughput screening assays to assess target engagement and functional activity.
- Generated robust data across multiple assay formats including fluorescence polarization, thermal shift, dual-reporter cell assays, and disease-relevant proliferation models.
- The platform confirmed selective target binding, demonstrated compound activity in a native cell context, and verified on-target pathway specificity using tool and test compounds.
DMPK & Toxicology Support
- Designed and executed a comprehensive in vitro ADME and DMPK profiling plan.
- Executed an extensive ADME screening program, completing >250 compound evaluations using a broad portfolio of in vitro assays such as solubility, microsomal/hepatocytes stability, Caco-2, CYP-time dependent inhibition, etc.
- Developed and validated a time-dependent CYP-inhibition assay, providing critical early insights into potential drug-drug interaction risks.
- Conducted both discrete and cassette PK studies, helping the client prioritise compounds based on bioavailability and clearance profiles.
- Supported early developmental toxicology studies in alignment with IND-enabling workflows.
- Carried out repeat-dose tox studies in both rat and dog models, integrated with cross-over formulation design to improve PK profiles.
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Conclusion - This integrated effort across medicinal chemistry, biology, DMPK, and toxicology demonstrates the impact of o2h's cross-functional discovery platform. Through close collaboration across disciplines, we enabled rapid lead optimisation, generation of high-quality screening data, and early risk assessment, all aligned with the client's preclinical development goals. Our multidisciplinary approach supported data-driven decision-making and efficient progression of the program from hit-to-lead through IND-enabling studies.
Accelerate your discovery with data-driven DMPK strategies tailored to your molecule. Let’s talk about how o2h Discovery can support your next project.
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To know more about our capabilities, please visit: https://o2hdiscovery.co. Want to stay informed about our latest discoveries, service offerings, and scientific initiatives? Follow o2h Discovery on LinkedIn and be part of the conversation.
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