Researchers at the Institute of Biochemistry at the Hebrew University have developed an innovative algorithm that "learns" the taste of drugs during the development process, thus warning against excessive bitterness
Will the drugs soon be tastier?
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The research effort in drug development is concentrated in the development of effective and safe drugs so that they can cure disease with a minimum of side effects.
However, there is a problem that does not get an optimal solution - the bitter taste of many drugs makes it difficult to take them orally.
Although introducing the drug into capsules usually solves the taste problem, this is a solution that is not always possible, as it increases the drug and may create real difficulty in swallowing.
While many are able to swallow the drug, despite its terrible taste or problematic size, there are populations that find it very difficult to do so, including toddlers and adults with difficulty swallowing.
Studies have shown that when there was a bitter taste to drugs, a decrease in responsiveness to treatment was observed in children - which posed a health hazard due to incomplete drug treatment.
For example, a study published in the Computational and Structural Biotechnology Journal found that over 90% of pediatricians report children who are unwilling to take medication because of their taste.
Because of the potential risks posed by the daunting taste of many drugs, the US FDA recently sought to add a flavor note to the list of side effects in child drug prescriptions, to warn parents of those problematic tastes.
But today, drug companies will recognize that there is a problem of very bitter taste only in the advanced stages of drug development, or in the clinical trials themselves, when the drug is given to thousands of people who serve as experimenters to test its effectiveness.
In case a particularly unusual taste problem is identified, companies will have to go back and change the composition of the drugs in order to try and screen the terrible taste (which is not always possible) - a process that will lead to further delays in drug release, millions of dollars in financial losses and other unwanted animal experiments.
Therefore, drug companies will usually prefer to launch a drug even if they have already realized that it is very bitter, in the hope that we will deal with the unbearable taste.
In the research group of Prof. Masha Niv, a taste researcher at the Institute of Biochemistry, Food and Nutrition at the Faculty of Agriculture, Food and Environment of the Hebrew University, they understood the severity of the problem, and were able to develop an algorithm that predicts strong molecule .
Eitan Margolis, a doctoral student in Prof. Niv's laboratory, talks about the research process and the process of creating the algorithm using a machine learning method regarding intense bitterness: "We collected molecules from a database set up in our laboratory and contain information on over 1000 bitter compounds. We received from our colleagues at the pharmaceutical company GSK and at the natural materials company AnalytiCon Discovery.
"Next, we taught the computer to understand which combinations of chemical properties are most important in order for a particular substance to be perceived as having a very bitter taste and thus 'trained' it to quickly identify whether a particular molecule might be very bitter or not. So we actually created the BitterIntense algorithm.
"After a performance test we saw that it is correct in over 80% of cases, which strengthens the potential for its use for the development of taste-friendly drugs - without the need for early synthesis of the substance and testing in humans or animals. In addition, since it is a computational model, we can continue to improve As more information accumulates about bitter molecules. "
And what about medicines for corona disease?
Margolis adds that "we have seen that the prevalence of highly converted drugs among those currently in development or approval for corona treatment is higher than in the general drug group. This result is interesting, as loss of taste is a very significant and common symptom among those infected with the virus."
In conclusion, the researchers believe that BitterIntense is a method that may reduce financial costs, animal experiments and shorten the time the drug reaches the consumer.
The ability to detect high bitterness in an integrative manner in the process of discovery and development, will help in the development of appropriate drugs for children and geriatric patients.
In addition, the algorithm is also relevant to biotechnology companies and companies that are working on the development of new sweeteners (sometimes also bitter) or natural ingredients that aim to be integrated into food products.