Biodistribution and Pharmacokinetic Analysis of RMT-Targeting Biologics
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Biodistribution and Pharmacokinetic Analysis of RMT-Targeting Biologics

Inquiry

The blood-brain barrier (BBB) is a major obstacle in developing therapeutics for central nervous system (CNS) disorders, as it restricts large and hydrophilic molecules from reaching the brain. Due to this low exposure level, biologics developed for CNS disorders often fail to achieve therapeutic concentrations at the site of action. Receptor-mediated transcytosis (RMT) offers a promising solution to deliver biologics across the BBB. RMT can enhance the brain uptake of biologics or carrier molecules that bind to endogenous receptors expressed on brain endothelial cells. Pharmacokinetic (PK) analysis and brain biodistribution assessment are essential steps in evaluating the potential success of RMT-targeting biologics. These studies support the development of more efficient RMT-based brain delivery systems by verifying that biologics reach the brain in sufficient concentrations for therapeutic action.

Whole-body fluorescence imaging in mice demonstrates distinct peripheral biodistribution patterns for ATVTfR, ATVCD98hc, and control IgG.
Fig. 1 Whole body mouse fluorescence imaging reveals unique peripheral biodistribution patterns of ATVTfR, ATVCD98hc, and control IgG. (Khoury, et al., 2025)

Our Services

At Ace Therapeutics, we specialize in providing comprehensive biodistribution and PK analysis services tailored for RMT-targeting biologics. Our advanced methodologies allow us to evaluate the efficiency of RMT-targeting biologics in reaching their target brain tissues and provide critical data to optimize RMT-based brain drug delivery systems.

PK Analysis of RMT-Targeting Biologics

  • Plasma and Brain PK Profiles
    We can help clients generate detailed in vivo plasma and brain PK profiles of RMT-targeted biologics administered intravenously (IV) or via alternative routes. These profiles allow us to analyze the absorption, distribution, metabolism, and excretion (ADME) characteristics of RMT-targeted biologics, providing crucial data to understand their bioavailability and brain exposure.
  • Calculation of Key PK Parameters
    We provide a range of essential parameters to analyze the pharmacokinetic properties of RMT-targeted biologics, including Cmax, Tmax, AUC, clearance (CL), volume of distribution (Vd), and half-life (t1/2).
  • Extended Brain Exposure
    Our PK studies also focus on helping clients validate whether modified and optimized drugs have a longer circulation time, particularly through FcRn-binding optimization or payload design modifications to increase brain exposure.

Assessment of Brain Distribution and Uptake of RMT-Targeting Biologics

  • Bioanalytical methods: We can use various bioanalytical techniques, such as ELISA-based bioanalysis, radiometric assays and detection, to quantify the concentrations of RMT-targeted biologics in whole brain, brain microvessels, brain extracellular fluid, and brain parenchyma.
  • Imaging techniques: We utilize cutting-edge imaging technologies, such as fluorescence and PET imaging, to verify the distribution of biologics across different brain regions. These studies provide detailed spatial analysis of the brain penetration of RMT-targeted biologics.

Advantages of Our Services

  • Comprehensive Analysis

We offer a full spectrum of PK and biodistribution services, providing a holistic view of RMT-targeted biologics in vivo, particularly their ability to cross the BBB and distribute in the brain.

  • Cutting-Edge Technology

Our state-of-the-art techniques, such as fluorescence imaging, PET imaging, and ELISA, provide reliable data to guide the development of RMT-targeted biologics.

With Ace Therapeutics' biodistribution and pharmacokinetic analysis services, we aim to provide clients with the critical data needed to develop their RMT-targeting biologics. Contact us today to learn more about our RMT-based brain drug delivery services.

Reference

  1. Khoury, N., et al. (2025). Fc-engineered large molecules targeting blood-brain barrier transferrin receptor and CD98hc have distinct central nervous system and peripheral biodistribution. Nature Communications, 16(1), 1822.
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