Naming of drugs

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Naming of drugs

• A marketed drug has three names a chemical name,
  a generic name, and a brand name.

• A chemical name is given when a new chemical
  entity (NCE) is developed.

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• The chemical name is a scientific name based on
  the compound's chemical structure (e.g.,
  6-thioguanine) and is almost never used to
  identify the drug in a clinical or marketing
  situation.
• Often, the name is long and difficult to
  pronounce, and, since it has numbers, the number
  in the name might become confused with the
  numbers in the prescription.

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• The generic name (or non-proprietary name) is
  granted by the USAN Council and is commonly used
  to identify a drug during its useful clinical
  lifetime.
• Link

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• The generic name does not belong to the company
  that discovers the drug (or owns the patent).
  Once the patent lifetime is expired, any company
  may market the drug under the generic name.

5

• The generic name must be screened to assure that
  it does not resemble any other generic or brand
  name.
• The generic name must also be appropriate for the
  class of drug.

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• A listing of appropriate drug stem names can be
  found in the National Library of Medicines Drug
  Portal
• The stems refer to the mechanism of action of the
  drug (not the disease condition)
• Link

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• The company that patents the drug creates the
  brand name (trademark). This name identifies the
  drug during the 17 years that the company has
  exclusive rights to make, sell, and use it under
  patent law.

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• Link
• Link

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History of the Pharmaceutical Industry

• Most of today's major pharmaceutical companies
  were founded in the late 19th and early 20th
  centuries.
• Key discoveries of the 1920s and 1930s, such as
  insulin and penicillin, became mass-manufactured
  and distributed (penicillin in WW II).
  Switzerlnd, Germany and Italy had particularly
  strong industries, with the UK and US following
  suit.

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• Legislation was enacted to test and approve drugs
  and to require appropriate labeling.
• Prescription and nonprescription drugs became
  legally distinguished from one another as the
  pharmaceutical industry matured.

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• Attempts were made to increase regulation and to
  limit financial links between pharmaceutical
  companies and prescribing physicians, including
  by the relatively new US FDA.
• Such calls increased in the 1960s after the
  thalidomide tragedy came to light, in which the
  use of a new tranquilizer in pregnant women
  caused severe birth defects.

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The Sulfanilamide Disaster

• In 1937, S. E. Massengil Company created an
  elixir (liquid form) of the antibiotic
  sulfanilamide using diethylene glycol as solvent.

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Ethylene Glycol
Diethylene Glycol

• Diethylene glycol is a great solvent, but
  extremely toxic.
• Unfortunately, at the time, there were no legal
  requirement to test the toxicity of the drug
• This resulted in the deaths of more than 100
  people in the U.S.

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• The United States Federal Food, Drug, and
  Cosmetic Act (abbreviated as FFDCA, FDCA, or
  FDC) was passed by Congress in 1938
• This law gives authority to the FDA to oversee
  the safety of food, drugs, and cosmetics.

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• Numerous new drugs were developed during the
  1950s and mass-produced and marketed through the
  1960s.
• This included the first oral contraceptive, The
  Pill, Cortisone, blood-pressure drugs and other
  heart medications. MAO Inhibitors, chlorpromazine
  (Thorazine), Haldol (Haloperidol) and the
  tranquilizers ushered in the age of psychiatric
  medication.

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• Valium (diazepam), discovered in 1960, was
  marketed from 1963 and rapidly became the most
  prescribed drug in history, prior to controversy
  over dependency and habituation.

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• In 1964, the World Medical Association issued its
  Declaration of Helsinki, which set standards for
  clinical research and demanded that subjects be
  given informed consent before enrolling in an
  experiment. Pharmaceutical companies became
  required to prove efficacy in clinical trials
  before marketing drugs.

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• Cancer drugs were a feature of the 1970s. From
  1978, India took over as the primary center of
  pharmaceutical production without patent
  protection.The industry remained relatively small
  scale until the 1970s when it began to expand at
  a greater rate. Legislation allowing for strong
  patents, to cover both the process of manufacture
  and the specific products, came in to force in
  most countries.

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• By the mid-1980s, small biotechnology firms were
  struggling for survival, which led to the
  formation of mutually beneficial partnerships
  with large pharmaceutical companies and a host of
  corporate buyouts of the smaller firms.
• Pharmaceutical manufacturing became concentrated,
  with a few large companies holding a dominant
  position throughout the world and with a few
  companies producing medicines within each
  country.

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• The pharmaceutical industry entered the 1980s
  pressured by economics and a host of new
  regulations, both safety and environmental, but
  also transformed by new DNA chemistries and new
  technologies for analysis and computation.
• Drugs for heart disease and for AIDS were a
  feature of the 1980s, involving challenges to
  regulatory bodies and a faster approval process.

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• Managed care and Health maintenance organizations
  (HMOs) spread during the 1980s as part of an
  effort to contain rising medical costs, and the
  development of preventative and maintenance
  medications became more important.
• A new business atmosphere became
  institutionalized in the 1990s, characterized by
  mergers and takeovers, and by a dramatic increase
  in the use of contract research organizations for
  clinical development and even for basic RD.
• 'Big Pharma' confronted a new business climate
  and new regulations, born in part from dealing
  with world market forces and protests by
  activists in developing countries.
• Animal Rights activism was also a problem.

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• Glaxo Wellcome SmithKline Beecham
  GlaxoSmithKline

Merger of Glaxo Wellcome and SmithKline Beecham
creates pharmaceutical giant Alison Abbott,
MUNICH, Munich JONNY EGGITT/FT Garnier to head
Glaxo SmithKline. The merger of the British
pharmaceutical companies Glaxo Wellcome and
SmithKline Beecham, which comes into effect this
summer, creates a giant which could rank number
one in the world in terms of spending on research
and development (RD). It will boast a portfolio
of 30 new drugs and 19 vaccines in clinical
trial. Glaxo Wellcome is currently the
fifth-largest pharmaceutical company in the world
in terms of turnover and SmithKline Beecham is
ranked twelfth. The new company will have a
stock-market value of 110 billion (US180
billion).
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• Marketing changed dramatically in the 1990s,
  partly because of a new consumerism.
• The Internet made possible the direct purchase of
  medicines by drug consumers and of raw materials
  by drug producers, transforming the nature of
  business.
• In the US, Direct-to-consumer advertising
  proliferated on radio and TV because of new FDA
  regulations in 1997 that liberalized requirements
  for the presentation of risks.

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• The new antidepressants, the SSRIs, notably
  Fluoxetine (Prozac), rapidly became bestsellers
  and marketed for additional disorders.

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• Drug development progressed from a hit-and-miss
  approach to rational drug discovery in both
  laboratory design and natural-product surveys.
• Demand for nutritional supplements and so-called
  alternative medicines created new opportunities
  and increased competition in the industry.

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• Controversies emerged around adverse effects,
  notably regarding Vioxx in the US, and marketing
  tactics.
• Pharmaceutical companies became increasingly
  accused of disease mongering or over-medicalizing
  personal or social problems.

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• There are now more than 200 major pharmaceutical
  companies, jointly said to be more profitable
  than almost any other industry, and employing
  more political lobbyists than any other industry.
  
• Advances in biotechnology and the human genome
  project promise ever more sophisticated, and
  possibly more individualized, medications.

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Industry revenues

• For the first time ever, in 2006, global spending
  on prescription drugs topped 600 billion, even
  as growth slowed somewhat in Europe and North
  America.
• Sales of prescription medicines worldwide rose 7
  percent to 602 billion, according to IMS health,
  a pharmaceutical information and consulting
  company.
• The United States still accounts for most, with
  252 billion in annual sales. Sales there grew
  5.7 percent.

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Top Pharmaceutical Companies (sales)
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Lipinskis Rules of Five
An orally active drug should have the following

• No More than five hydrogen bond donors
• No more than ten hydrogen bond acceptors
• A molecular weight under 500 daltons
• An octanol-water partition coefficient less than 5

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How many drug targets are there?
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What classes are important?
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Assigned Reading

• Gundersen L The complex process of naming drugs.
  Annals of internal medicine (1998), 129(8),
  677-8.
• http//www.medscape.com/viewarticle/469843
• (you will need to create a free medscape account,
  and to click on the box at lower right to see all
  4 sections)
• http//www.fda.gov/AboutFDA/WhatWeDo/History/Produ
  ctRegulation/SulfanilamideDisaster/default.htm
• Hopkins Andrew L Groom Colin R The druggable
  genome. Nature reviews. Drug discovery
  (2002), 1(9), 727-30.