Roxadustat

2023-04-04:

Roxadustat (FG-4592) #

• Hypoxia-inducible Prolyl Hydroxylase inhibitor, thus promoting HIF-1α/HIF-2α.
  • See also FG-4497.
• Elevated endogenous EPO by 2x
• Possible blood pressure increase - was not found in metanalyses and only in a small minority in clinical trial.
• Erythropoiesis gives a performance advantage due to additional oxygen capacity but too much over time can potentially become problematic if it leads to polycythemia. There should be low risk with roxadustat as it was shown to be safe in healthy men, but if you already have high rbc, hemoglobin, hematocrit or are on anabolic steroids for example(in which case you shouldnt use it anyway), the risk would be increased.
• The HIFα-Stabilizing Drug Roxadustat Increases the Number of Renal Epo-Producing Sca-1+ Cells
• Roxadustat: Not just for anemia
  • In particular, it has the potential to increase the risk of pulmonary hypertension and vascular calcification, and aggravate inflammatory infections.
    • However, this is just based off a single case study of a diseased 73 year old woman, lol.
    • [Evaluation of the Carcinogenic Potential of Roxadustat (FG-4592), a Small Molecule Inhibitor of Hypoxia-Inducible Factor Prolyl Hydroxylase in CD-1 Mice and Sprague Dawley Rats]
• Roxadustat prevents Ang II hypertension by targeting angiotensin receptors and eNOS
  • HIF-1α inhibits AT1 and activates AT2 and eNOS.
• FG-4592 Improves Depressive-Like Behaviors through HIF-1-Mediated Neurogenesis and Synapse Plasticity in Rats
  • HIF-1α -> CREB, BDNF, EPO, VEGF obviously, but also PSD-95 and Homer-1.
• Hypoxia inducible factor stabilization leads to lasting improvement of hippocampal memory in healthy mice
• Thyroid Hormone Receptor β agonist and slightly less affinity for α (for all I know T3 might be similar).
  • ROXADUSTAT-INDUCED HYPOTHYROIDISM: THE EFFECT OF ROXADUSTAT ON SUPPRESSION OF THYROID FUNCTION
    • TSH and T4 drop.
  • Effect of Roxadustat on Thyroid Function in Patients with Renal Anemia
  • Roxadustat and thyroid-stimulating hormone suppression
    • Decrease in TSH, T4, and T3.

Dose #

• Everychem: $45 for 1.5g ($30/g). So $3 per 100g dose, which is brootal.
• Or, 5g for $109 ($21/g) on Umbrellalabs. $2.18 per 100g dose.
  • Not bad; basicaly the price of 2 jars (3g) on EC
• https://libreddit.hu/r/NooTopics/comments/12m5je1/roxadustat_dosing_schedule/
  • Seems studies use something like 50-70-120mg 3x/week.
• Neanderthulean took 100mg 4-5 days a week. Snorted 70mg and found it very unpleasant.
  • Yeah I think I’ll do 100 mg on almost every workout day. All things considered, the endurance improvement will probably save me >30 minutes a week not resting and fucking around; just getting in the zone.
• Intranasal should be best for brain selectivity; its penetrance isn’t the best. But I’m not sure it’s pleasant. The shit’s also green btw.
• EPO peaks 8 hours after dosing.