RE: QSAR - Were half of the current drugs discovered prior to 193 0?

From the article "The Other Side of Drug Discovery" at the web site,
http://www.bio.com/newsfeatures/newsfeatures_features.jhtml?action=view&cont
entItem=49623739&Page=1
you can find some answers of your questions:

I just cited here:

**************beginning of the citation*******************
While there are around 10,300 FDA-approved drugs in the United States today,
most of these are made up of some combination of only 433 distinct
molecules. Acetaminophen, for instance, is an ingredient in hundreds of
separate drugs. Half of the 433 were approved before 1938, and at least 50
are "me too" drugs, a slightly modified form of compound already on the
market. Finally, there are only eight major, chemical "scaffolds" upon which
all the 433 molecules are based.
"All this says," says Bartfai, "is that it is darned hard to make a new
molecule that is going to be a drug these days."
****************End of the citation***********************

It would be interesting to know at what Tanimoto Index we can get 433
classes from 10,300 FDA-approved drugs (if someone knows where we can get
these structures). From here we can also trace back how many classes have
drugs before 1938. However, I am afraid there will be some tricks to further
narrow down these classes into eight major chemical "scaffolds".

Any comments?

Shi-Yi
-----Original Message-----
From: kubinyi*t-online.de [mailto:kubinyi*t-online.de]
Sent: November 14, 2002 12:35 PM
To: qsar_society{:}accelrys.com
Cc: kubinyi,+,t-online.de
Subject: Re: QSAR - Were half of the current drugs discovered prior to
1930?

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---
Dear all, 
although I do not have figures at hand, I would like to share some
comments with Yvonne and you.
First, who is Professor Bartfai? Is he an expert in the field?
Second, how is the term drug defined? Does acetaminophen, because it is
present in 200 different formulations, count 200 times? Is opium a
"drug", as we define a drug nowadays, or is it just a bioactive plant
product? Morphine started 1806, a most-often used synthetic analog,
Tramadol, only some decades ago. Penicillin was discovered more than 70
years ago, was isolated and introduced into therapy about 60 years ago
- but broadband, orally active, lactamase-resistant analogs were
developed less than thirty years ago. Aspirin was discovered in 1897,
introduced into therapy in 1899, but its mechanism of action and its
powerful activity as an antiaggregation drug was dicovered only in the
early seventies. The COX-2 selective drugs celecoxib and rofecoxib were
introduced in the market in 1999.
Third, do we count all drugs that have ever been used during the last
hundert years or only those that are still in the market? Or do we only
count the drugs that are of any importance, nowadays?
I propose that we take only the last criterium and, in this respect,
much more than fifty percent of all "relevant" drugs are from the last
thirty years. If we look at sales, this percentage is even more
impressive - but this might be an unfair argument because patented
drugs are in general much more expensive than patent-free drugs.
The million dollar question is: does anybody have exact figures?
Best regards
Hugo 
yvonne.c.martin_+_abbott.com schrieb:
> Hi all,
> 
> I received the following e-mail and have been able to
> trace this only to a 
> talk given by Prof. Bartfai. 
>
http://www.bio.com/newsfeatures/newsfeatures_features.jhtml?action=view&cont
entItem=49623739&Page=1
> 
> Does anyone have more information? Do you want to
> question this statement?
> 
> Yvonne
> ----- Forwarded by Yvonne C Martin/LAKE/PPRD/ABBOTT on
> 11/14/02 09:16 AM 
> -----
> 
> 
> James B Summers
> 11/14/02 08:10 AM
> 
>  
>         To:     Yvonne C Martin/LAKE/PPRD/ABBOTT
>         cc: 
>         Subject: 
> 
> Heard an interesting statement in a presentation
> yesterday.  Have you ever 
> seen this statement or know the author:
> 
> ?       There are 10,300 medicines but they come only
> from 433 distinct 
> chemical entities half of which were discovered prior to
> 1930
>           (ref: T. Bartfai, The Scripps Research
> Institute)
> 
>
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