Chemistry International
Vol. 23, No. 2
March 2001
Two
Routes to Becoming a Medicinal Chemist
by
C. Robin Ganellin **
Introduction
|
Prof. C. Robin Ganellin (University
College London)
|
For the purposes of this article and the published references
cited at the end, medicinal chemistry is considered in the context
of the pharmaceutical industry, where it is concerned with the discovery
and synthesis of compounds for biological evaluation as potential new
drug therapies. It embraces the identification, design, synthesis, isolation,
and chemical characterization of such compounds, the study of structure-activity
relationships, and the molecular and physicochemical basis for biological
activity.
How to become a medicinal chemist? This question is of interest to
many aspiring chemists wishing to become professionally involved in
the design and synthesis of potential new drug molecules. The pharmaceutical
industry is where most new chemical entities are developed into therapeutic
products. It is a major employer of organic and medicinal chemists.
There are two main routes to becoming a medicinal chemist. The most
direct is by formal university courses at both undergraduate and postgraduate
levels. The less direct and less certain is to train initially as an
organic chemist and then join a pharmaceutical company engaged in new
drug discovery and learn what is required "on the job". This route may
take many years, and the outcome is uncertain. Probably not even the
majority of organic chemists following this industrial route to medicinal
chemistry will successfully make the transition to becoming a medicinal
chemist making decisions about drug design.
View of Big Pharma
A few years ago, the IUPAC Medicinal Chemistry Section (now part of
Division VII, Chemistry and Human Health) decided to find out from industry
what was their preference for taking on new employees who will become
their medicinal chemists. A questionnaire was sent [1]
to leading medicinal chemists and research directors in the major international
pharmaceutical companies engaged in research and development; their
responses were surprisingly similar. Over 90% of the answers indicated
that they preferred to take on organic chemists rather than specialists
in medicinal chemistry. Some did suggest that it would be helpful for
staff to have had some acquaintance with biological subjects such as
biochemistry, pharmacology, and physiology [2-4].
It was very strongly stated that the most important educational background
required of the new chemists was excellent training in synthetic organic
chemistry and that most other necessary skills could be learned on the
job. Surprisingly little interest was shown for having chemists with
formal academic training in medicinal chemistry, or for chemists trained
in organic synthesis but also having significant education in biological
subjects.
Clearly, this finding must reflect the view that "if you cannot make
the compound, then you cannot test it". However, what the chemist selects
to make is also very critical; so, presumably, the opinion must exist
that there are already sufficiently experienced medicinal chemists present
in the companies to assist new chemists in the selection of target compounds.
The balance required between these aspects of expertise and the ease
of acquiring expertise is obviously debatable.
Academic Route
Historically, formal university education in medicinal chemistry takes
place primarily in faculties or schools of pharmacy. There, medicinal
chemistry is only one of a variety of subjects taught at the undergraduate
level, where the primary focus is on education for future practicing
pharmacists.
Undergraduate medicinal chemistry is usually taught by academic staff
(i.e., faculty members) who are practicing medicinal chemists in the
sense that they are usually supervising postgraduate students involved
in studying a medicinal chemistry topic at research level, often for
a Ph.D. requirement, and/or postdoctoral researchers. It was of interest,
therefore, to find out where such academically research-trained medicinal
chemists fit into the job spectrum of professionally active medicinal
chemists. To this end, a questionnaire was sent to medicinal chemistry
professors in faculties or schools of pharmacy in eight countries, including
France, Germany, Italy, Japan, Spain, Switzerland, the United Kingdom,
and the United States. The questionnaire aimed to elicit information
about postgraduate medicinal chemistry students, their courses and training,
and the occupations taken up after graduation. The replies representing
109 medicinal chemistry departments or sections have been analyzed,
and the results have been published [5-7]
to provide a database on modern medicinal chemistry curricula for comparative
purposes. The information should help guide discussion of the appropriate
paths to be followed by students in preparation for their careers.
The above countries were selected because they have many faculties
or schools of pharmacy and a developed pharmaceutical industry with
a history of drug discovery. Some other countries with excellent drug
discovery traditions, such as Belgium, Denmark, the Netherlands, and
Sweden, were not canvassed because they possess few faculties of pharmacy.
The questionnaire consisted of 15 main questions and was divided into
three sections. The first section was aimed at eliciting information
about the composition of the post-graduate student body and the nature
of the positions taken by the students after completing their studies.
The second section requested information about the faculty staff. The
third section asked about student coursework. The reader is referred
to the publications for details.
Discussion
It was apparent that the training of medicinal chemists equips them
to enter a wide range of occupations. In some of the countries, a substantial
proportion of medicinal chemists do continue into synthetic medicinal
chemistry. This pathway is especially evident in France, Japan, and
the United Kingdom. On the whole, the numbers entering industry also
look reasonably healthy and contrast interestingly with the expressed
preference for organic chemists received from those with responsibility
for hiring in the industry. The gulf between industry and academia as
judged by the responses does not appear to be so wide. The impression
given by the answers to the questionnaire sent to big pharmaceutical
companies was that they were not particularly interested in hiring medicinal
chemists. Presumably, fewer medicinal chemists are required to select
drug targets and to influence structure-activity analysis in comparison
with the number of chemists needed for synthesis who may be working
together on a team. In addition, a proportion of the organic chemists
will become medicinal chemists by experience "on the job" helped by
short courses [8]. Furthermore, many more
organic chemists than medicinal chemists are trained in universities;
perhaps the ratio is >10:1. So it is easier for companies to find
good organic chemists for drug synthesis, in comparison with the relatively
few medicinal chemists available.
Big pharmaceutical companies, especially, organize drug discovery in
teams of specialists, and they seek the best specialists available.
All these factors contribute to create the overall impression that big
pharmaceutical companies do not especially seek medicinal chemists for
drug discovery. This trend may not apply to the many small pharmaceutical
companies engaged in drug research who do not have teams of specialists
and who have to rely much more on generalists. The latter may be medicinal
chemists who understand organic synthesis but at the same time know
how to converse with biochemists, pharmacologists, and other biologists.
Possibly, small companies may be where the many trained synthetic medicinal
chemists find their employment. In any case, the evidence is that the
academic training of medicinal chemists equips them to enter a wide
range of occupationsmany of which are in industryand that
medicinal chemists are able to find suitable jobs.
References and Notes
1. The questionnaire was sent out in 1996 and 1997.
2. W. D. Busse and C. R. Ganellin. In Trends in Drug Research, Pharmacochemistry
Library, V. Claasen (Ed.), Vol. 20, pp. 305-315, Elsevier, Amsterdam
(1998).
3. C. R. Ganellin, L. A. Mitscher, J. G. Topliss. In Annual Reports
in Medicinal Chemistry, Vol. 30, pp. 329- 338, Academic Press, New York
(1995).
4. W. D. Busse, C. R. Ganellin, L. A., Mitscher. Eur. J. Med. Chem.
31, 747-760 (1996).
5. C. R. Ganellin, L. A. Mitscher, B. Clement, T.-H. Kobayashi, E. Kyburz,
O. Lafont, A. Marcincal A. Monge, G. Tarzia, J. G. Topliss. Eur.
J. Med. Chem. 35, 163-174 (2000). Online at <http://www.iupac.org/divisions/VII/761_1_90/report_EJMC2000.html>
6. C. R. Ganellin, L. A. Mitscher, J. G. Topliss. Med. Res. Rev. 18,
121-137 (1998).
7. T.-H. Kobayashi and C. R. Ganellin. Medchem. News 8, 21-28 (1998).
8. C. R. Ganellin. "Syllabus for a short postgraduate course in medicinal
chemistry", Chem. Int. 17, 212- 214 (1995). Online at <http://www.iupac.org/divisions/VII/761_1_90/syllabus_mc.html
** Prof. C. Robin Ganellin (University
College London, Department of Chemistry, Christopher Ingold Laboratory,
20 Gordon Street, London, England WC1H OAJ, UK; E-mail: [email protected]),
Titular Member of the IUPAC Chemistry and Human Health Division (VII)
Committee, President of the Medicinal Chemistry Section (VII.M) Committee,
and Titular Member of the Medicinal Chemistry Section Commission on
Training and Development (VII.M.2).