Yeah, sure, I'll take a shot (FWIW).
<<NZYM responded by saying that while they do address a niche market, focusing on one year of product launches probably gives a skewed view of the market for peptide-based drugs. They believe the potential pipeline to be a bit richer than the less than 10% that TD suggested. >>
OK, how about 1999? According to Volume 35 of "Annual Reports", 33 small molecule NCEs were introduced last year. A grand total of 5 are in any way "peptidic" or amino-acid derived. Out of those five, Cetrorelix (Asta Medica) has some cool amino acids, but Synercid is just a 70:30 ratio of two established semi-synthetic antibiotics. CHF-1301 is simply the methyl ester of L-DOPA. Eptifibatide (another anti-thrombotic, interestingly) has six very natural amino acids, while the antidiabetic nateglinide is simply an acylated version of phenyl alanine.
So, while there are indeed 15% NCEs containing amino acids this year, only one (3%) would have been a candidate for using NZYM's expertise. So, combined with my reading of the literature, I am very comfortable with a figure of 10% or so. (So?)
<<The company went on to say that combinatorial chemistry is founded on "multi-functional amino acids." So medicinal chemists are also trying synthetic amino acids in analogs of peptide and peptidomimetic small molecule candidates. >>
Combinatorial chemistry of course WAS founded on amino acid (i.e., peptide) chemistry. But I certainly hope the NZYM rep did not mean to imply that a majority, or even a significant minority, of the combichem going on today is amino-acid based. Quite simply, it is not. Scanning any recent combichem journal will back up that claim.
<<NZYM suggested that genomics based drug discovery could well result in the flow of more peptide and protein based compounds into development>>
I will buy that, though there obviously no data to support it. Certainly the peptide part. But will those peptides be recombinant or synthetic? And if they're protein based, most if not all will use natural amino acids (don't see that benefitting NZYM). Does NZYM have any contact with Gryphon? This is a private company that makes large proteins synthetically. Now THAT might prove an interesting combination!!
<<It is even possible that amino acid derivatives could be used as chiral building blocks in compounds that don't approximate a peptide much at all.>>
That is completely correct. But there are many ways of making such derivatives. NZYM would have to compete with those technologies. Maybe they can. But chiral catalysis is very popular . . .
<<I believe Dan mentioned that NZYM is trying to be more proactive in searching the biotech universe for folks who could use their products, rather than waiting for hits on the product page of their website or for the phone to ring. >>
Good for them. I had never heard of them until I wandered into the NZYM thread on SI. Haven't bought a thing from them. I have bought amino acids from Aldrich, Sigma, NovoBiochem, and the like. But, really, why are they concentrating on biotech? That's probably not where the big money is. Many of the best biotech-discovered drugs will likely be developed by big pharma anyway.
<<I'm no medicinal chemist, but I feel a little better about the current situation, >>
And here I'll quote myself right back at you:
<<they really only need a few base hits to make it, so it's possible>>
Best of luck, |
