Human Dose Prediction

Human dose prediction is recognized as an important parameter in IND-enabling drug discovery program. Creative Biolabs validates human dose combined with in vitro and in vivo methods. We are able to predict human dose and Cmax for new drugs. Besides, risks in early human dose are able to rank, identify, and flag.

The oral route is one of the most commonly used modes of delivering drugs. For oral drugs, a dose needs that causes blood concentration exceeding a certain potency level for an agreed time period to be predicted. We predicted the dose based on a series of parameters. These parameters should be measured in PK studies during the lead optimization phase. In addition, a drug's physicochemical characters, ADME and Time-kill properties can be of great value in highlighting particular parameters and help dose prediction.

With our extensive experience and highly devoted experts, we take into account several in vivo parameters, which including but not limited to:

  • Maximum concentration (Cmax)
  • Minimum concentration (Cmin)
  • Time of maximum concentration (Tmax)
  • ADME parameters [clearance (CL), volume of distribution (Vz), protein binding, absorption, permeability]
  • Area under concentration-time curve (AUC)
  • Half-life (t1/2)

As a replacement for in vivo studies, Creative Biolabs also provides you in vitro prediction method to estimate a credible human efficacious dose. Using an appropriate combination of data sources, an in vitro method is faster than an in vivo one and could achieve prediction as soon as the compound is firstly synthesized. In vitro prediction could predict dose within only days rather than weeks or months, opening the way for better and faster decision-making. Besides, the volume of testing of in vitro studies is lower than in vivo studies, which save you a lot of time and budget. Most importantly, in vitro methods have no ethical problem with animal usage, which is cruel and unaccepted for many researchers. Supported by our state-of-the-art in vitro ADME studies, we measure data of Cmax, Cmin, CL, fraction of an oral dose absorbed from the gastrointestinal tract, protein binding (fraction unbound in blood, fraction unbound in the microsomal or hepatocyte incubation, fraction unbound in plasma), volume of distribution and QSAR to set a prediction model. The outcome of our in vitro model is the best predictions.

Human Dose Prediction Figure 1. Predicted human doses using in silico input data including the AstraZeneca Development compounds validation data set and other candidate drugs (Page 2016)

We offer different approaches to set an initial effective concentration in human and to predict human dose. Our in vivo and in vitro approaches have been shown to have real potential in producing credible dose estimates. For more detailed information, please feel free to contact us or directly sent us an inquiry.

Reference

  1. Page KM (2016). “Validation of Early Human Dose Prediction: A Key Metric for Compound Progression in Drug Discovery.” Mol Pharm 13(2): 609-620. doi: 10.1021/acs.molpharmaceut.5b00840.


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