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Biotech Medicine News Science

FDA Unveils Biosimilars Guidance 30

ananyo writes "The U.S. Food and Drug Administration has released its long-anticipated draft guidance for drug makers interested in making generic forms of biological drugs such as enzymes and antibodies. The move could open the door for cheaper versions of some of medicine's most expensive drugs, but it is still unclear how many companies will be willing to tackle the challenges and uncertainties of making 'biosimilar' drugs. Copying biological molecules is a stickier proposition than making ordinary generic medicines because proteins are typically much larger and more complex than small molecule drugs. They are also often produced in cell cultures, and even small variations in how the cells are grown can change the properties of the protein produced."
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FDA Unveils Biosimilars Guidance

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  • by TWX ( 665546 ) on Friday February 10, 2012 @10:00PM (#39002647)

    I'm confident that even with expensive and difficult processes it'll still happen. Look at some of the treatments for Chron's Disease- there's a med that a friend of mine uses that's massively complex and extremely expensive, but allows her to essentially live a normal life. It's thousands of dollars a month, so something half the price could still be very profitable if it still works properly.

    Certainly a lot of generics manufacturers might avoid the more complex drugs, but plenty will take a look, and possibly new companies will get in on the act too.

    • by Anonymous Coward

      Have a look at filgrastim, and the epoetins - there are already some biosimilars on the market, or at least there are in the UK. Interestingly, the original filgrastim (from Amgen) is the cheapest of all of the options in the UK (there are alternatives from Teva, Sandoz, Ratiopharm and Hospira). However, this is actually because the presence of multiple biosimilars has brought the price of all of the options down - when there were only two biosimilars, in 2010, one of the biosimilars was the cheapest option

    • by Anonymous Coward

      Interesting example since there is a drug used off label that is very cheap LDN (low dose naltraxone) that the NIH studied and treats Chron's very well. It has been around since the 60's and was used to treat opiate addiction in higher doses. I hope this info helps your friend.

      • by Anonymous Coward

        Naltraxone is not a adalimumab substitute and causes liver damage. Adalimumbb (Humira) is a Tumor Necrosis Factor blocker. Adalimumab is a "biologic", Naltraxone is a small molecule drug.

        • by Anonymous Coward

          This is good news for me.
          I was on Humira for over a year for my psoriatic arthritis. I went from being barely able to walk to pain free in 36 hours after my first shot. It's about $1500 a month for the drug but it was so worth it. Unfortunatly my overactive immune system decided to go after the Humira so it doesn't work anymore. I guess it's time to try Enbrel, which works on the receptors instead of the protien. As it is now I'm taking over a gram a day of Nalprelan just to manage pain and swelling an

    • by TheLink ( 130905 )
      If I had Crohn's Disease and the cheap stuff didn't work well, and they suggest kilobux per month treatment, I'd seriously consider fecal/stool transplants.
  • Seems to me... (Score:2, Interesting)

    by jamstar7 ( 694492 )
    If you want biological molecules for drugs, the last thing you want to do is try to synthesise them Why not just open up yeast to genetic engineering and have the modified yeast create your molecules by the ton? Once you have the research and modifications done, you can grow those yeasts for pennies.
    • Re:Seems to me... (Score:5, Informative)

      by jonwil ( 467024 ) on Friday February 10, 2012 @10:46PM (#39002787)

      If you read the summary, it says they are already producing these molecules via cell cultures.

      A protein is a VERY complex molecule and simply inserting a gene into a yeast strain might not produce a protein that is similar enough to what humans make to be viable as a drug.

    • Re:Seems to me... (Score:4, Informative)

      by Anonymous Coward on Friday February 10, 2012 @11:01PM (#39002827)

      Yeast is used sometime, but a lot of drugs, insulin for example, are made by modified E. Coli. It's not as simple as just using the human DNA sequence in the bacteria since bacteria cannot remove the introns and stitch together the extrons that are in the human sequence. How you get around this issue differs by manufacturer. [http://www.enotes.com/insulin-reference/insulin] Additionally, most diabetics don't use Regular insulin, which would use the normal human sequence, but insulin lispro, which goes by the brand name Humalog, or one of the equivalent fast-acting insulins. The reason for this is because diabetics are injecting the insulin either with needles or an insulin pump, the insulin needs to be absorbed from the subcutaneous layer (fat layer below the skin), so Regular insulin wouldn't actually be absorbed the same way it is when a non-diabetic's pancreas secretes the insulin. Humalog also works faster (within 5 minutes) instead of the 30 minutes of Regular, so it allows a diabetic to give insulin right before or directly after eating and have the insulin work almost as fast as a non-diabetics insulin response.

      • Regular (and NPH) insulins have the advantage of being out of patent for over 10 years and not requiring prescription in most (all?) states. That's not the case with analogs, although I believe the patent on Humalog runs out next year.

        And actually, yeast is used in the production of insulin, Novo Nordisk's Novolin [nih.gov] insulin, for instance. Extraction is easier, but production is lower. However, research published in 2010 [microbialc...tories.com] (open access) describes techniques for significantly boosting the production using a
    • Re: (Score:2, Informative)

      by Anonymous Coward

      Why not just open up yeast to genetic engineering and have the modified yeast create your molecules by the ton? Once you have the research and modifications done, you can grow those yeasts for pennies.

      I had a car ride last week with someone who regulates this kind of business. In the case of normal drugs, with a relatively simple active ingredient, it's pretty easy to prove that your generic drug is identical to the original name-brand drug that went through all the clinical trials to satisfy the regulators. So, the regulatory process for generic versions of simple drugs is comparatively simple

      For biological drugs, though, the molecules are generally too complex to replicate exactly. Generic companies

    • Re:Seems to me... (Score:5, Insightful)

      by Guppy ( 12314 ) on Saturday February 11, 2012 @01:43AM (#39003257)

      If you want biological molecules for drugs, the last thing you want to do is try to synthesise them Why not just open up yeast to genetic engineering and have the modified yeast create your molecules by the ton? Once you have the research and modifications done, you can grow those yeasts for pennies.

      I'm sorry, but this is an example of a +4 moderated comment that doesn't know what it's talking about, and does not understand the basic gist of the regulatory issue that this article is dealing with.

      Nobody is synthesizing anything, biopharmaceuticals are by definition substances (non-small-molecule) derived from biological organisms, whether engineered or naturally occurring. A bit of explanation: Small molecule drugs (like say, asprin) are chemically simple. As such, it is easy to demonstrate equivalence of a generic to the original; you show all your chemical bonds are in the right place, and that your formulation is rolled up in a pill that gets absorbed the same, those kinds of tests are sufficient for approval.

      But biomolecules were treated differently, for the reason that it was impossible to do the same kind of analysis -- an analysis could find all testable parameters exactly the same, but things would work differently simply because it came out of a different manufacturing process. So there were no "generic" biologicals. A second company could copy something like say, Amgen's erythropoetin protein -- but although an identical protein, it would be considered a separate drug, and go through a new approval process just like it was a brand-new drug.

      Generic companies have long clamored to allow biologicals to be treated the same as chemical entities,skipping the extremely lengthy and expensive process of doing clinical trials and such again. And of course, the originator companies argued that bio-similars should go through safety trials, too (as they could not be conclusively proved to be identical to the original). So, we had a regulatory tug-of-war running for the past... two decades or so, that has finally been settled (or so it seems at the moment).

      As for the various issues of production via various types of organisms is something I don't want to get into right now, but let's just say we're dealing with techniques far more sophsticated than yeast expression these days.

    • by Anonymous Coward

      I work in this field so I can give better details on at least one example of the problem. You do grow these products cheaply, exactly like you were thinking.

      Many of these drugs are based off antibodies, which has a carbohydrate portion that is not defined in the DNA and can drastically change the effects. Grown in E.coli (very cheap), there will be no carbohydrate attached and the antibodies will not activate the immune system. Yeast will attach carbohydrates, but different ones than a mammalian cell, so

    • And the real cost of manufacturing is not from the genetic adaption of the cells and their growth, but is in the purification. After the cell has replicated and grown all the protein (Mol wgt 3,000 - 15,000) you want, you have to extract it from the chemical soup that exists in the cell. The cells are ground up and then filtered physically and chemically to separate out the one protein you're interested in. With antibodies the situation is often more complex because of there extreme uniqueness (which is
  • Biologicals comment (Score:5, Informative)

    by Guppy ( 12314 ) on Saturday February 11, 2012 @01:17AM (#39003191)

    For pharmaceuticals, small-molecule drugs and biologicals have long been regulated under two different tracks, for reasons both historical and practical (including the problem that biologicals simply aren't amendable to the kind of complete analysis you can do on small molecules). Sometime ago (maybe about a decade or so?) back, the FDA decided to modernize things, and start applying principles from the former track to the latter. There were a lot of facilities that used processes little-changed since being invented back as far as the 50's and 60's, that were shuttered; recent product and vaccine shortages happened not long after the number of manufacturers dwindled (for some products, from double-digits down to 1-2 sources).

    Anyway, wanted to give an example of the limitations of characterizing biologicals. A while back, there was a case involving an Erythopoetin drug (used to treat certain kinds of anemia). The FDA mandated a change in manufacturing, in a big push to get rid of animal-derived raw materials (in this case, anything bovine-derived, following the mad-cow scare). The protein drug in the new formulation was found to be exactly the same by every testable parameter -- sequence, folding, everything else -- and seemed to function the same when examined in animal and human subjects. But when it was released for use in the field, there was a sudden spike in cases of pure red blood cell aplasia (where the body simply stops make any RBCs). Little details in the manufacturing process can sometimes make an enormous difference.

    To use an analogy, biologicals are sometimes like arcane and kludgy code that nobody fully understands; once you somehow get it working, there is good reason to not to poke it, and to fear that it might break in somebody else's hands.

  • by ComputerPhreak ( 1057874 ) on Saturday February 11, 2012 @02:03AM (#39003321)
    Anecdotally, a lot of people (including many who are well-educated about the pharmacology behind drugs) swear there is a difference between some generic and brand drugs, and between the different generics. Sure, most of the time it's a placebo effect, but there are legitimate factors that can cause real differences, such as different binders and fillers being used, that can change the rate of absorption of the active ingredient, or even cause unrelated side effects or affect the bioavailability of the active ingredient. It will be interesting to see if these new, more complex molecules will widen the (perceived or real) differences between brand and generic medications.
  • by mauthbaux ( 652274 ) on Saturday February 11, 2012 @10:15AM (#39004729) Homepage
    Since there seems to be a bit of confusion here, allow me to explain (inadequately I'm sure) why different manufacturing processes for biologics result in non-identical molecules even though the DNA sequence and folding of the amino acids is the same.

    One of the primary differences is in the glycosylation of the protein. This is where sugar groups of various structures are attached to the outside of the protein and act as a sort of label to the body (distinguishing self from non-self proteins), and even within the cell itself (identifying where the protein should be placed inside of the cell). Different organisms each have their own system for attaching and interpreting these sugar groups. For instance, typical yeast Saccharomyces cerevisiae has a glycosylation profile that will cause the human immune system to attack it eventually - which will make you have an adverse reaction not only to the drug that you're taking, but any other drug produced in the same organism. The yeast Pichia pastoris has a glycosylation profile that is superficially similar to a human one, making it less likely to cause an adverse reaction, but the organism is locked down by patents. Furthermore, there's some evidence that the glycosylation is affected by the health of the cells in the culture, and the media that you're culturing them in. Frequently we'll just coat the proteins in polyethylene glycol and hope for the best.

    The other place that variation occurs is in the purification processes that are used to separate the drug molecules from everything else. Many of the purification processes will alter the glycosylation profile or the folding of the protein. They're also generally rather lossy, in that the purer the protein you want, the less of it you'll end up with, and the more it will cost. We used to attach tags to the proteins so that they were easier to purify (his6 was a common one), but then there were concerns that the tag itself would become the target for an immune reaction (which, like the glycosylation, would make a person resistant to not only the drug they were taking, but any other drug that used the same tag), so the practice has been mostly discontinued.

    The simple fact is that biologics will always result in mixed batches of molecules, and different manufacturing processes do directly affect that mix. The trick for biosilmilars will be to ensure that their mix is functionally similar enough to the original one; which will likely require clinical trials - meaning that cost savings won't be nearly so drastic as it is with small molecule drugs. While we've figured out how to make DNA translate to a protein of our choosing, we're not nearly as knowledgeable about how to manipulate sugar groups in a similar manner. Progress is being made for sure, but we're not there yet.
  • I got to interview the Salk Institute's Ronald Evans about exercise, training, and fitness -- he's a cell biologist and looks at how drugs might mimic the *signals* of exercise without a person actually exercising. In fact, there's a good candidate: the drug AICAR does just this, making cells believe they've exercised without all the, you know, sweating and such. The body ramps up its burn rate and you lose weight and gain muscle. Unfortunately, Evans says not to look for AICAR anytime soon -- it's generic

Keep up the good work! But please don't ask me to help.

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