Lead optimization
Combining in vivo profiling and software for confident lead optimization
EVIDENCE-DRIVEN DECISIONS, HUMAN-RELEVANT
More predictive than traditional animal models.
TARGET POTENCY THRESHOLDS
Know how much the potency should be improved in LO for a clinically viable drug.
LOWER DEVELOPMENT RISK
Avoid costly cycles optimizing doomed compounds.
RATIONAL, DATA-DRIVEN OPTIMIZATION
No more blind modifications.
POTENTIAL REGULATORY ADVANTAGE
Humanized model data strengthens your preclinical package.
Do you have a compound in this phase?
Which TAD services can help you to move forward?
Early lead PK/PD in TADHuMouse®-Pfalc
A dose fractionation, dose-response, PK/PD study with your early lead to know a) the PK drivers of efficacy of the chemical family, b) the frequency of resistance in vivo, c) the potency to cure P. falciparum in TADhuMouse® and, d) the first Total Human Dose estimate
Main outcomes
Parasite stage susceptibility and speed of action in vivo
What type of medicine will the program produce?Frequency of resistance in vivo
Is resistance a liability of the project?
Potency for antimalarial efficacy in vivo
How much potency to aim at to be competitive in Total Human Dose?
Testing new drugs in LO against the early PK/PD function
Are we losing the mechanism of action in LO?
Are we gaining potency in LO?
TADmaps® comparison with standard antimalarials from TAD historical dataset
How does the project compare with standards?
Test drug-induced liabilities because of hemotoxicity
(i.e., G6PD)
Is the LO program mitigating this liability?
