4 ms·

"Esketamine" is just the S-isomer of ketamine (thus "S-ketamine"), which has conventionally been an equal ("racemic") mixture of the S- and R-isomers. It's not

"Esketamine" is just the S-isomer of ketamine (thus "S-ketamine"), which has conventionally been an equal ("racemic") mixture of the S- and R-isomers. It's not so much that they've changed anything about the drug as that they've isolated the variant which is more psychoactive.

randomacct3847 8y ago
Ok - but just isolating the active part of the drug makes it patentable. Still ridiculous given how cheap Ketamine is.
- marssaxman 8y ago
  It is completely ridiculous. S-ketamine has been available on the black market for years - it's not like anything about this is rocket science.
  - mirimir 8y ago
    If that's true, maybe their patent is invalid. But maybe there's also a patent on the delivery mechansim. Or maybe it's a process patent.
    - loeg 8y ago
      Sure; we know they have a valid patent or else it would not have been worth their time to bring the drug to market.
      - mirimir 8y ago
        Seriously? Janssen obviously believes that it's valid. Or at least, they're confident that they can defend it. Maybe they know that it's not valid, but are confident that others won't figure out why. In one case that I recall, the manufacturer bribed a chemist to retract a paper that had reported the synthesis of their drug. Many years of budget cuts have rendered the Patent Office pretty clueless about drugs. And the FDA doesn't do any independent assessment of patent validity. I've seen testimony where FDA staff said that they lack expertise for that. So basically, patents are valid if they survive litigation.
        rjf72 8y ago
        It's not just budget cuts. It's an exploding legal system behind patents. Try to decipher the patent rules [1] sometime. It's filled with incredibly counter-intuitive self referential legalese that, even when one understand the jargon, is not entirely clear. And it regularly has very major changes made to the entire code. In general as you approach some degree of complexity in anything, the number of individuals who sufficiently grasp it approaches 0. And then as you're mentioning - that's only about the patent legalese itself. Now the patent examiners also need to be able to have an understanding of what are ideally novel new inventions in various fields, which themselves are often increasingly obfuscated. Anybody could perform a sufficiently capable of job this has way better career opportunities than earning $80k at the patent office. While this does support your notion of budgetary cuts being the primary problem, again I think that misses the core problem which is that the system has become so convoluted that actually having a meaningful holistic understanding requires immense skill and education. Systems that are supposed to be for public, and individual, use should not require a juris doctor to begin to parse. The whole system needs a major overhaul, frankly like much of our formal structures. Isn't it a bizarre system that people are expected to completely obey laws which they are in no way expected to be able to completely understand? [1] - https://www.uspto.gov/web/offices/pac/mpep/index.html https://www.uspto.gov/web/offices/pac/mpep/index.html
        loeg 8y ago
        It's valid because USPTO approved it, yes. We're first-to-file, not first-to-invent now.
        mirimir 8y ago
        True. But there's still the on-sale bar: > "A person shall be entitled to a patent unless . . . the claimed invention was patented, described in a printed publication, or in public use, on sale, or otherwise available to the public before the effective filing date of the claimed invention."[0] 0) https://www.whitecase.com/publications/alert/supreme-court-says-america-invents-act-did-not-alter-sale-bar https://www.whitecase.com/publications/alert/supreme-court-s...
mirimir 8y ago
Right. And unless the inactive R-isomer has some negative effect, it's a meaningless change.
- refurb 8y ago
  Ketamine isomer (S+) induces less drowsiness, less lethargy and less impairment in clustered subjective cognitive capacity than equianalgesic small-dose racemic ketamine. In addition, S(+) ketamine causes less decline in concentration capacity and primary memory [Pfenninger et al. 2002]. The S(+) isomer of ketamine has about twice the analgesic potency of the clinically used racemic mixture. Therefore, the known side effects may be reduced when one half of the usual dose is administered. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4910398/ https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4910398/
  - mirimir 8y ago
    Thanks. But if S(+) ketamine has been commercially available, even if only illegally, it's not patentable.
    - AstralStorm 8y ago
      Not quite, the specific purification process may or may not be patentable.
      - mirimir 8y ago
        True. Process patent. But those are harder to defend in litigation, as I recall.
- AstralStorm 8y ago
  R isomer is quite active too and similarly, which is why nobody bothered with purified S isomer.

randomacct3847 8y ago

Ok - but just isolating the active part of the drug makes it patentable. Still ridiculous given how cheap Ketamine is.

marssaxman 8y ago
It is completely ridiculous. S-ketamine has been available on the black market for years - it's not like anything about this is rocket science.
- mirimir 8y ago
  If that's true, maybe their patent is invalid. But maybe there's also a patent on the delivery mechansim. Or maybe it's a process patent.
  - loeg 8y ago
    Sure; we know they have a valid patent or else it would not have been worth their time to bring the drug to market.
    - mirimir 8y ago
      Seriously? Janssen obviously believes that it's valid. Or at least, they're confident that they can defend it. Maybe they know that it's not valid, but are confident that others won't figure out why. In one case that I recall, the manufacturer bribed a chemist to retract a paper that had reported the synthesis of their drug. Many years of budget cuts have rendered the Patent Office pretty clueless about drugs. And the FDA doesn't do any independent assessment of patent validity. I've seen testimony where FDA staff said that they lack expertise for that. So basically, patents are valid if they survive litigation.
      - rjf72 8y ago
        It's not just budget cuts. It's an exploding legal system behind patents. Try to decipher the patent rules [1] sometime. It's filled with incredibly counter-intuitive self referential legalese that, even when one understand the jargon, is not entirely clear. And it regularly has very major changes made to the entire code. In general as you approach some degree of complexity in anything, the number of individuals who sufficiently grasp it approaches 0. And then as you're mentioning - that's only about the patent legalese itself. Now the patent examiners also need to be able to have an understanding of what are ideally novel new inventions in various fields, which themselves are often increasingly obfuscated. Anybody could perform a sufficiently capable of job this has way better career opportunities than earning $80k at the patent office. While this does support your notion of budgetary cuts being the primary problem, again I think that misses the core problem which is that the system has become so convoluted that actually having a meaningful holistic understanding requires immense skill and education. Systems that are supposed to be for public, and individual, use should not require a juris doctor to begin to parse. The whole system needs a major overhaul, frankly like much of our formal structures. Isn't it a bizarre system that people are expected to completely obey laws which they are in no way expected to be able to completely understand? [1] - https://www.uspto.gov/web/offices/pac/mpep/index.html https://www.uspto.gov/web/offices/pac/mpep/index.html
      - loeg 8y ago
        It's valid because USPTO approved it, yes. We're first-to-file, not first-to-invent now.
        mirimir 8y ago
        True. But there's still the on-sale bar: > "A person shall be entitled to a patent unless . . . the claimed invention was patented, described in a printed publication, or in public use, on sale, or otherwise available to the public before the effective filing date of the claimed invention."[0] 0) https://www.whitecase.com/publications/alert/supreme-court-says-america-invents-act-did-not-alter-sale-bar https://www.whitecase.com/publications/alert/supreme-court-s...

mirimir 8y ago

Right. And unless the inactive R-isomer has some negative effect, it's a meaningless change.

refurb 8y ago
Ketamine isomer (S+) induces less drowsiness, less lethargy and less impairment in clustered subjective cognitive capacity than equianalgesic small-dose racemic ketamine. In addition, S(+) ketamine causes less decline in concentration capacity and primary memory [Pfenninger et al. 2002]. The S(+) isomer of ketamine has about twice the analgesic potency of the clinically used racemic mixture. Therefore, the known side effects may be reduced when one half of the usual dose is administered. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4910398/ https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4910398/
- mirimir 8y ago
  Thanks. But if S(+) ketamine has been commercially available, even if only illegally, it's not patentable.
  - AstralStorm 8y ago
    Not quite, the specific purification process may or may not be patentable.
    - mirimir 8y ago
      True. Process patent. But those are harder to defend in litigation, as I recall.
AstralStorm 8y ago
R isomer is quite active too and similarly, which is why nobody bothered with purified S isomer.