Fluorine atoms have a unique combination of electronic and physical properties. As such, when incorporated into active pharmaceutical ingredients (APIs), fluorine atoms often influence their protein binding affinity and lipophilicity but not the shape of the resulting fluorochemicals. Fluorination can thus significantly impact the bioavailability or metabolic stability of drug substances.
The pivotal role that the element fluorine plays in modulating the properties of bioactive molecules is reflected by the growth of its presence in approved drugs, as evidenced by the fact that between 15% to 20% of all medicines and agrochemicals on the market contain at least one fluorine atom in their structure. As of 2009, the FDA had approved >140 fluorine-containing drugs, such as fluorouracil, Miglitol, Gemcitabine, Sofosbuvir, atorvastatin, fluoxetine, ciprofloxacin, etc.
The judicious introduction of fluorine into a molecule can productively influence conformation, pKa, intrinsic potency, membrane permeability, metabolic pathways, and pharmacokinetic properties.
Nowadays, the application of specialty fluorochemicals in the pharmaceutical industry has been increasingly widespread. TargetMol’s fluorochemical library has become an effective tool for developing new anticancer drugs, anesthetics, antidepressants, antifungals, antiviral drugs, antibiotics, cholesterol lowering agents, and anti-inflammatory agents. In addition, in agricultural uses, the addition of fluorine to many agricultural herbicides, pesticides, and fungicides improves the potency and therefore reduces the required application rate of these substances.
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