Open up ”a lost field” in Drug Discovery

It is no doubt that we get a lot of benefits from drugs, and a lot of new medicine has given medical professionals the opportunity to give help and advice to patients. However, some influential people such as the CEOs of pharmaceutical companies and leading drug researchers are saying recently that the discovery of new drugs is becoming harder than before. This is because the process needs increasingly more advanced technology and a huge amount of money as evidenced by EBM (evidence based medicine). Interestingly, management critics of drug companies have intended to make recommendations to mergers and acquisitions to a giant corporation few years ago, however, the situation is dramatically changing. Indeed, today's leading role of R&D has taken the place of small venture companies that focus on their speciality utilizing intelligent and efficient staff. Moreover, there are some researchers, who play an active part in new medical innovations in small business, are refocusing their target on the most advanced biological drugs, vaccines and tissue engineering in high specialty fields. At present, these individuals are gradually developing into excellent entrepreneurs, thus their principle for a drug discovery is a practically reasonable approach. However, I am discovering “a lost field” that will open up new approach for drug discovery. That is an application called “reverse innovational approach”1) to create harmony of small molecules and the bio-networks system2).

Today, there is a surprising commoditization of low molecular weight compounds in drug discoveries. The interesting background of the commoditization is that, thanks to the development of organic chemistry, the hardships related to drug discovery are becoming more manageable. In other words, there are many players who struggle to create new drug candidates from various fields, they can easily create a lot of new chemical compounds in a very good laboratory condition with high knowledge of organic chemistry. Therefore, we could have a golden opportunity to get a lot of new compounds for drug candidates. However, in the place of medical chemistry, some obstacles have appeared on the stage for drug discovery. It is especially becoming more and more difficult to discover new candidates of low molecular weight compounds because of the two following reasons. One is to be clear of some barriers of drug's character3) for human body; “Lipinski's rule of five” is a very famous rule of thumb to evaluate druglikeness of small molecules. Now, the rule has become an indispensable precondition for a standard process of drug discovery in modern systematic approach. If it is so, there would be restrictions of synthetic spaces to adjust to the rule when we try to discover druglikeness candidates in small molecules. The other is a hindrance of the patentable approach for new drug candidates. Of course, a patent is a very important system for drug companies and inventive people, on the other hand, the system restricts access to new drug discovery for third-party resarchers. In other words, there are a lot of small molecules that are listed in material patents, the third-party could not be within easy access for appropriate examinations of the drug candidates for the period of patent. In the long run, the approach for synthetic space of druglikeness-molecules becomes narrow and limited.

Next, I will introduce improvement drugs (me-too drug). The definition is that their structure is very similar to already known drugs, however, their characteristics are not exactly the same. The mimicry characteristic such as slight differences of functional groups lead to some unique peculiarities in medicinal action and pharmacokinetics. From my experience of medicinal chemistry for new drug discovery, the peculiarities are very noteworthy because they decide new characteristics of the drug in the human body. For example, a small optimization of molecule structures will dramatically improve their characters, the methods are useful guidance for new drug candidates. Moreover, the improvement drugs may have potential to have an easy approach for “essential drugs”4). Disappointingly, there is gradually little intention to develop improvement drugs because of hardly receive approvals, exclusive patents and promotion of generic drugs. However, historically essential drugs had competed with each other and improved through the market mechanism of trial and error. In addition, there were the principle of competition among improvement drugs for next generation in efficacy, safety and price reduction. Thus, there may be plenty of room of a newcomer to discover a new approach.

Now, I suggest a new approach of reverse innovation of the combinational drugs with bio-networks system2). As mentioned above, there is room for business chances of drug improvement, so I will make a proposal to create harmony between improvement drugs with digital networks. What is more, the new approach will give new chances to encourage “combinational drugs”2) , which are defined as innovative chemistry between low molecular weight compounds, medical devices and body parts. In addition, the approach will produce new opportunity to create new value for third-party drug discoverers in overall three positions; effectiveness, safety and patentability. In my opinion, the process to improve existing drugs would desirably be the most suitable approach for developing countries because a improvement drug has similar characteristics to already known drugs, the cost for their development would be low, if its patent would be opened or licensed out at a low fee. Therefore, there are some merits for developers to create new combinational products using improvement drugs with bio-networks strategy. In this strategy, drugs, such as improvement drugs, become new bio-materials for a component of combinational drugs. Thus, it will produce new approach for drug discoveries. In the end, the strategy will be a hub of medical digital signals in harmony with the new bio-materials, therefore it will produce a lot of useful business opportunities among many various creators with low start-up costs.

Reference

1) https://hbr.org/2015/07/engineering-reverse-innovation

2) https://nmtbaron.amebaownd.com/

3) Drug's character; if a chemical compound with a certain pharmacological or biological activity has properties that would make it a likely orally active drug in humans., CA Lipinski, Adv. Drug Del. Rev. 1997, 23, 3. (https://en.wikipedia.org/wiki/Lipinski%27s_rule_of_five)

4) WHO Model List of Essential Medicines