If someone has the time to dig deep and find out exactly why the the tablets have a film coating that would be really helpful. I have searched but not found anything yet.
I asked Dr. Oracle
The film on trametinib dimethyl sulphoxide tablets serves a critical purpose in maintaining the stability and efficacy of the medication. Its primary function is to:
Protect the tablet from moisture exposure
Preserve the dimethyl sulfoxide (DMSO) content of the tablet
Bioavailability Preservation
DMSO content is crucial for maintaining trametinib bioavailability
Loss of DMSO can adversely impact the drugās effectiveness ([1])
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Great info! Can you ask Dr. Oracle how they get around this issue with the liquid formulation of trametinib?
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jnorm
#122
Storage in an amber glass vial should work fine. [ref]
Now you guys have me digging through enteric coating patents to learn how to coat my own tablets.
*Not medical advice. Consult a compounding pharmacist and patent lawyer. 
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āComparative Bioavailability of a Single Dose of Trametinib (TMT212) Containing 9% vs 11% Dimethyl Sulfoxide in Randomized Healthy Volunteers to Assess LongāTerm Storage at Room Temperatureā
This study was sponsored and funded by Novartis Pharmaceuticals Corporation.
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FWIWā¦
A 70-75% solution of DMSO will give you the best absorption through the skin.
.5mg per ml trametinib /DMSO{70-75%] solution, topical on the radial artery on the wrist, closest artery to the skin surface.
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J0hn
#126
Thank you Joseph, thatās an interesting paper thatā¦.
These results indicated that storage of trametinib at room temperatures ā¤25Ā°C during the overall shelf life of 36 months would not negatively impact trametinib bioavailability.
ā¦opens up the possibility of ordering from India, if the refrigeration requirement for storage/shipping is removed.
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Unfortunately, the references cited by Dr. Oracle are behind paywalls. I am only listing two of many citations
Conclusion
Developing a stable liquid formulation of trametinib requires a multifaceted approach. By leveraging ionic liquid technology, optimizing formulation parameters, and employing protective strategies, it may be possible to create a liquid trametinib product that maintains stability without the need for a protective film coating.
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Do any of the Indian pharmacies you guys regularly order from carry 0.5mg Trametinib? Anil doesnāt have it.
The pricing I quoted earlier is from Maulik, who can get it for you:
Maulik at Shreeji Impex (ShreejiImpex.com
maulik7@gmail.com
whatsapp: +91 9925171777
website: www.shreejiimpex.co.in
@Shreeji_impex - username for telegram app
If you end up pursuing this, let me know. It would be good to get a standardized set of lab tests / blood tests to do before and afterwards to help identify any side effects of low doses.
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Iām talking with Maulik and he confirmed that the Trametinib would be shipped at normal temperature, likely for 10-15 days. Itās a cold storage product, so Iām wondering if this could be an issue, ie either make the med less effective or potentially toxicā¦
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Report from Kamil (a scientist at NSU in Singapore) on ARDD:
In recent years The Aging Research and Drug Discovery Meeting has ascended as one of the most important aging conferences.
All your ERK are belong to us
This ARDD, Linda Partridge presented her work on the combination of trametinib and rapamycin. Trametinib is a MEK inhibitor that leads to reduced MAPK/ERK signalling and synergistic lifespan extension with rapamycin under some circumstances ā even in F1 mice that pass the 900-day rule.
Hopefully they will pursue phase I studies soon, because I know for certain that we and others are interested in proper microdosing of trametinib. At the same time the ITP updated their webpage and announces that trametinib is in the ITP (which we knew through the grapevine). Interestingly, even Widaja et al. 2024 showed that pERK phosphorylation is up with aging and that this can be reduced by an anti IL-11 antibody, although I do not fully trust that data because I have rarely seen such strong anabolic upregulation with aging before. Be that as it may, an MAPK/ERK inhibitor is clearly an excellent choice to inhibit ERK!
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Unfortunately Maulik informed me today that Trametinib is not available for exportā¦
@RapAdmin are you aware of any other exporters from India that would send the 0.5mg Trametinib?
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Pender
#134
Summary of the Kaeberlein video: he doesnāt think the tranetinib + Rapamycin study will replicate because the controls didnāt live very long (700-800 days).
His rule of thumb is mouse studies need controls to have around a median 900 day lifespan in order to trust results showing a lifespan extension.
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After seeing Kaeberleinās video I see no reason to jump on the trametinib bandwagon.
To paraphrase Dr. Blagasklonny, āanythingā plus rapamycin appears to be better than āanythingā alone.
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Already in the hopper:
https://www.nia.nih.gov/research/dab/interventions-testing-program-itp/supported-interventions
Yes. When compared to studies with normal-lived controls, the rapa + trametinib male mice did no better than control animals in other studies, and the females did no better than high-dose rapa alone, and substantially worse than strict CR:
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RapAdmin
#137
ah yesā¦ the kaeberlein test
source x.com
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vamin
#138
I think itās a good rule of thumb in general but Iāll bet this one replicates. This isnāt a simple test/control, there was a control, trametinib, rapamycin, and the combo. Not only did trametinib and rapamycin outperform the (short-lived) controls, but the combo outperformed rapamycin and trametinib alone. Itās not just a one-off result, itās a trend. If you donāt believe the control group is valid, you can drop them and still come to the conclusion that the addition of trametinib improves lifespan over rapamycin alone.
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