Rapamycin, Rapamune, Sirolimus and Other Naming Conventions

Rapamycin has had many names associated with it, including brand names like Pfizer Rapamune, and the generic drug name sirolimus. And there are many different branded generic versions rapamycin. Read on to learn about all the different companies that make rapamycin, and the names they use to refer to it.

Rapamycin was initially investigated as an anti-fungal, but then it was found to have immunomodulation properties (it can decrease or increase the immune system function). It was ultimately approved for the prevention of allograft rejection in recipients of organ transplants.

In addition to this application, preclinical and early clinical studies showed that rapamycin alone and in combination inhibited tumor cell proliferation, suppressed tumor angiogenesis, and induced apoptosis (cell death) of some cancer cells.

However, as the patent on rapamycin was about to expire and extensions were being reviewed, it was no longer financially feasible to continue its development as a cancer therapeutic. As such, other mTOR inhibitor products began to be developed that could be patented.

Rapamycin was first approved for sale by the FDA in 1999. The patent for rapamycin expired in 2013 and the first generic version of the medication became available in the USA in 2019.

Since it was first discovered, companies have put their own brand names on their products, and a generic drug name “sirolimus” was established.

Here is a listing of the different names rapamycin is known by:

Rapamycin
Generic Name: Sirolimus

Brand Names:

  • Pfizer Rapamune
  • Wyeth Rapamune

Generic Manufacturers of Rapamycin / Sirolimus:

  • Glenmark Pharmaceuticals Sirolimus
  • Zydus Siromus
  • Biocon Rapacan
  • Rocas Sirolimus
  • Panacea Biotec - Siropan sirolimus
  • Actiza Sirolimus
  • Dr. Reddy’s Sirolimus

There are also drugs that are identified by the general term “Rapalogs” (a word formed from the “Rapa” from rapamycin, and “analogues” which in a compound with a molecular structure closely similar to that of another). These drugs that function virtually identically to the way rapamycin works (ie. targets the same receptors) and therefore have the same functional benefits.

Researchers have modified the structure of rapamycin to prepare numerous analogues, typically so that they can patent it for sale as a small molecule drug. In theory these drugs should provide the same life extension benefits as rapamycin, but this has not yet been confirmed in studies with animals.

The two main rapalogs on the market today are:

The patent on Novartis Afinitor (everolimus) has expired and generic versions of the drug are now approved and starting to become available at low cost.

Generic Manufacturers of Everolimus:

  • Glenmark Pharmaceuticals - Evermil (Everolimus) Tablets (5mg and 10mg)
  • Zydus Everomus (Everolimus) - (5mg and 10mg)
  • Biocon Evertor (Everolimus): tablets are available in 2.5 mg, 5 mg, 7.5 mg and 10 mg
  • Cipla Rolimus (Everolimus)
  • Natco Rampact Everolimus
  • BDR Pharmceutical Ltd Everbliss (Everolimus) - 5mg, 10mg
  • Bruck Pharmaceuticals Afilimus (Everolimus) - 5mg
  • Beacon pharma, Xevirol (Everolimus 5mg)
  • Hikma Everolimus, 2.5mg, 5mg, 7.5mg, 10mg
  • Par Pharmaceuticals Everolimus, 1mg, 2.5mg, 5mg, 7.5mg

All of these drugs are what are classed as MTOR inhibitors - drugs that block the MTOR1 pathway, and can also disrupt the MTORC2 pathway if used at high doses for long periods of time. Currently it is generally believed that most of the lifespan benefits come from inhibiting MTOR1, and most of the negative side effects of the medications from blocking MTOR2 - but this remains an active area of research.

Companies working on developing a new generation of MTOR inhibitors include:

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The brand of generic rapamycin (sirolimus) that I am getting from my pharmacy is from Dr. Reedy’s Pharmaceuticals/India. So, you can add Dr. Reedy’s to your list of generic suppliers of sirolimus. Ross

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Do you know of any test results for this brand of sirolimus? I.e, both potency and freedom from contaminants.

You did not provide the name of the brand you are asking about…???

I think he’s talking about your reference to Dr. Reddy’s sirolimus. I have not seen any lab test purity / potency tests on the Dr. Reddy’s sirolimus product.

https://www.drreddys.com/media/press-releases/oct28-2014.html

No…I do not know of any test results…but I have been suggesting that someone needs to compare the absorption and plasma levels of generic brands with Rapamune.

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Sorry for my ambiguous question. At the time of posting, I was interested in Zydus Siromus. But after seeing the list of ingredients, I switched plans and decided to see if I could get a pure sirolimus powder without dyes, polyethylene glycol, titanium dioxide, etc., and containing only sirolimus and a benign filler such as cellulose. I plan to get it from Tailor Made Compounding. I’ll ask them for a certificate of analysis to see if they’re willing to provide one.

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Just be aware of concerns around the bioavailability of the compounding pharmacy powder / capsules. There seem to be some issues. Best to do some blood testing (blood sirolimus level testing) after dosing to validate that its getting into your system: Bioavailability of Rapamycin From Compounding Pharmacy

Search on “sirolimus blood test” here on this site to get links to where you can get them.

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Yes, thank you, I learned of the poor bioavailability issue a couple weeks ago from this site. After learning about that, I read about sublingual rapa powder or else making a transdermal cream. I read some articles on the web about transdermal creams and am considering Phlojel which contains isopropyl palmitate, lecithin, water, and a polymer. I will also likely put a little menthol-containing oil in the mix such as eucalyptus oil, since that is reputed to be a penetration enhancer. And I just read your post about getting an affordable sirolimus blood test recently made available by Life Extension Foundation Lab services, so I can find out if either approach works.

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I would check out their reviews. Usually when a company has bad reviews from people who have reviewed many places, but only good reviews from people with 1 review, that is something to consider.

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Without specific reference to their sirolimus (in fact, specific drug names are blacked out in some public documents), Dr. Reddy’s has been a quality nightmare for at least seven years.

Indian drug firms struggle with quality issues: Chemical & Engineering News

Dr. Reddy’s Recalls Prescription Drug Blister Packages Due to Risk of Poisoning

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