Target Engagement in Topical Drug Development: Lessons from Tirbanibulin
Topical delivery of small molecules enables targeted treatment of skin diseases while minimising systemic exposure. However, clinical success requires more than passive skin penetration. Effective therapies need to achieve sufficient drug concentrations at the site of action, avoid local metabolism, and have sufficient residence time to enable target interaction.
Integrating medicinal chemistry, dermal pharmacokinetics, and formulation strategy is essential to improve clinical success rates. Formulation design also plays a central role, influencing absorption, distribution, and tolerability.
The presentation will use Tirbanibulin as a case study to show how integrating medicinal chemistry, dermal pharmacokinetics, and formulation design can overcome skin delivery challenges, achieve high local drug concentrations with minimal systemic exposure, and ensure consistent pharmacodynamic effects.
Topical Drug Delivery in Preclinical Research: Navigating Promise and Complexity
Topical drug delivery presents a promising strategy in drug development, offering direct access to the site of action while bypassing the gastrointestinal tract and hepatic first-pass metabolism. This targeted approach reduces systemic exposure and minimizes adverse effects. Despite its advantages, the discovery of drug candidates suitable for topical administration involves complex ADME challenges, including transdermal absorption and the need for simple formulations for screening NCEs.
In one of our integrated drug discovery programs, we employed a topical delivery system as a mitigation strategy to address toxicity concerns. This approach not only enhanced safety profiles but also demonstrated the practical utility of topical administration in early-stage drug development.
Why Watch the Webinar?
- Learn from real-world case studies in topical drug delivery
- Understand the ADME complexities in preclinical models
- Gain insights into formulation strategies that drive clinical success
- Interact with industry leaders and ask your questions live
Speakers
Miquel Salva
Miquel, Executive Director of DMPK at Syngene, has 30+ years in life sciences and biopharma. He previously led DMPK and preclinical development at Almirall and contributed to multiple US/EU-approved drugs. He holds a PhD in Biochemistry from Universitat Autònoma de Barcelona.
Vishwottam Kandikere, Ph.D
Dr. Vishwottam Kandikere is a global clinical pharmacokineticist with 25 years of experience. He has contributed to 13 NCEs, holds 11 US patents, and has authored over 90 publications. His work spans therapeutic areas such as neuroscience, oncology, and metabolic disorders. He has successfully led the discovery and optimization of 13 NCEs from bench to early clinical trials. Dr. Kandikere holds a Ph.D. in Pharmaceutical Analysis from Jawaharlal Nehru Technological University, Hyderabad.
Ashwani Gaur
Ashwani Gaur, Assistant Director and Site Head of DMPK at Syngene Hyderabad, has 20+ years of expertise in bioanalysis and LC-MS-based quantification across diverse biological matrices. He previously held roles at Ranbaxy, Advinus, and Eurofins, and holds an M.S. in Pharmaceutical Analysis from NIPER, India. He has contributed extensively to global drug discovery programs, particularly in lead identification and optimization stages, collaborating with both large and mid-sized pharmaceutical companies.
