Pharmaceuticals–Some Important Drugs - Fundamentals of Industrial Chemistry: Pharmaceuticals, Polymers, and Business - page 183

CHAPTER 11

Pharmaceuticals-Some
Important Drugs

11.1 INTRODUCTION

The FDA approves an average of just over twenty new drugs (New Molecular
Entities (NME) per year; in fiscal year 2011 there were 35 new drugs
approved. Today there are several thousand approved drugs. There are
hundreds of drug targets and many diseases require different and highly
specific medications. Most of the drugs are small molecules and most of
these are heterocycles [1]. The synthesis of different drugs is complex, often
requiring stereoselectivity and has been the subject of several topics [2 - 4].
A comprehensive discussion of this topic would require several volumes and
is beyond the scope of this text.
Although most drugs are based upon small molecules, there is an increas-
ing number of large molecule biologics. For example, adalimubab (Humira ® ,
Abbott), the number one biologic therapy, is made from recombinant DNA
technology and has over 1,000 amino acids and a molecular weight of approx-
imately 148 kd [5]. T lymphocytes (T cells) are a type of white blood cell
that release cytokines that promote the destruction of tissues surrounding the
joints. One cytokine is tumor necrosis factor ) and adalimubab is

a TNF blocker. Because of this, it is prescribed for rheumatoid arthritis and
several other indications. In 2011, 585,000 patients were treated with Humira
and sales were $7.9 billion [6]. Other biologics that are also TNF blockers
include etanercept (Enbrel ® , Amgen Inc.), infliximab (Remicade ® , Janssen
Biotech, Inc.), certolizumab pegol (Cimzia ® ) and golimumab (Symponi ® ,
Janssen Biotech, Inc.).
To give the reader the general flavor of the topic of pharmaceuticals, sev-
eral classes of drugs are illustrated. The groups were chosen because of their
importance in preventing disease and for the number of people that need the

α (TNF α