Name: MK2866(Ostarine) 100x10mg
Brand: Averlane Labs
Price: 65.00 EUR
Availability: InStock

NOT FOR HUMAN CONSUMPTION

MK2886(Ostarine) is an oral, non-steroidal selective androgen receptor modulator (SARM) designed to deliver anabolic effects in skeletal muscle and bone with comparatively less stimulation of prostate/skin than testosterone. It binds the androgen receptor (AR), drives ARE-regulated transcription, does not aromatize or undergo 5-α reduction, and shows tissue-selective co-activator recruitment. Enobosarm is not FDA/EMA-approved and is prohibited by WADA as an anabolic agent.

Additional Benefits of Enobosarm Now Under Investigation

Benefit	Key take-aways
1 Lean-mass and function (human signals)	Phase 2 studies in older/postmenopausal adults showed dose-dependent fat-free-mass gains (~1–1.5 kg over 12 wks) and improved stair-climb power/leg strength vs placebo. <br/><em>Journal of Clinical Endocrinology & Metabolism; Journal of Cachexia, Sarcopenia and Muscle</em>
2 Anti-catabolic protection	In disuse/illness models, enobosarm preserves myofiber CSA and lowers MAFbx/MuRF1 expression, attenuating muscle loss during immobilization or glucocorticoid exposure. <br/><em>FASEB Journal; American Journal of Physiology–Endocrinology</em>
3 Bone-anabolic signals	Rodent osteopenia studies show ↑ BMD, improved trabecular microarchitecture, and stronger three-point bend metrics with limited prostate stimulation. <br/><em>Journal of Bone and Mineral Research; Bone</em>
4 Cancer cachexia (mixed outcomes)	Phase 2 trials reported FFM and performance benefits in NSCLC/other cancers; Phase 3 (POWER)missed primary endpoints overall but suggested responsive subgroups, ongoing phenotyping work. <br/><em>JCSM; The Oncologist</em>
5 AR-positive ER⁺/HER2⁻ breast cancer	As a selective AR agonist, enobosarm shows antitumor activity in AR-enriched ER⁺ disease and is being explored alone or with CDK4/6 inhibitors. <br/><em>Cancer Research; Annals of Oncology</em>
6 Sarcopenic obesity & rehabilitation	Oral dosing adds to resistance-training gains and may speed post-hospitalization recovery, needs definitive RCTs. <br/><em>Geriatrics & Gerontology International; Sports Medicine</em>
7 Physical performance & QoL	Improvements in stair power, chair-rise, gait speed and patient-reported outcomes parallel anabolic changes in small studies. <br/><em>MSSE; Quality of Life Research</em>
8 Erythropoiesis (modest)	AR engagement can slightly raise hemoglobin/hematocrit, typically less than testosterone, monitor in at-risk patients. <br/><em>Hematology; Andrology</em>
9 Oral convenience	Once-daily oral dosing and ~24-h half-life support adherence relative to injectables. <br/><em>Clinical Pharmacology & Therapeutics</em>

2. Molecular Mechanism of Action

2.1 Receptor Pharmacodynamics

Enobosarm binds AR → nuclear translocation → ARE activation. In muscle, it up-regulates mTOR/S6K/4E-BP1 and local IGF-1, and down-shifts atrogenes; in bone, it promotes osteoblastogenesis (Wnt/β-catenin/Osterix) and may secondarily reduce resorption.

2.2 Down-stream Biology

Pathway	Functional outcome	Context
AR → mTOR/S6K	↑ protein synthesis, myofiber hypertrophy	Skeletal muscle
AR → Wnt/β-catenin/Osterix	↑ osteoblast activity, ↑ BMD	Bone
↓ FoxO/ubiquitin ligases	↓ proteolysis (MAFbx/MuRF1)	Catabolic stress
Myostatin/activin cross-talk	Shifts toward anabolism	Muscle

3. Pharmacokinetics

Route: Oral, once daily.
Half-life: ~24 h (steady state ~5–7 days).
Absorption: Good oral bioavailability; minimal food effect.
Metabolism: Hepatic oxidative/conjugative pathways; high protein binding.
Elimination: Renal/hepatic excretion of metabolites.
Doping: Long-term metabolites enable detection weeks after discontinuation.

4. Pre-clinical and Translational Evidence

4.1 Healthy/Older Adults

Phase 2 trials: lean-mass increases with favorable trends in strength/power and physical function; reversible HPG suppression and HDL lowering observed.

4.2 Oncology

Cachexia: Mixed, benefits in body composition/performance in Phase 2, Phase 3 overall negative on primary function endpoints.
Breast cancer: AR-positive ER⁺ cohorts show clinical activity signals; combinations with CDK4/6 inhibitors under study.

4.3 Orthopedics/Rehab

Early translational efforts pair enobosarm with progressive resistance training to shorten time-to-function after immobilization or surgery.

Evidence quality note: Human datasets are short- to mid-term and modest in size; long-term efficacy/safety outcomes (CV events, fractures, prostate/breast endpoints) remain unresolved.

5. Emerging Clinical Interests

Field	Rationale	Current status
Sarcopenia/frailty	Oral anabolic with tissue selectivity	Phase 2 signals; larger RCTs needed
Cancer cachexia	Appetite-neutral anabolism vs ghrelin mimetics	Mixed; subgroup strategies
AR-positive ER⁺ breast cancer	AR agonism as antitumor strategy	Ongoing studies
Osteopenia/osteoporosis adjunct	Bone-anabolic + anti-resorptive balance	Preclinical/early human
Rehabilitation	Faster strength/function recovery	Pilot concepts

6. Safety and Tolerability

Endocrine: Dose-dependent LH/FSH and testosterone suppression (men); menses/ovarian axis effects possible in women, generally reversible post-stop.
Lipids: HDL-C reductions (often 10–20%); occasional ↑ LDL/TG, monitor CV risk.
Hepatic: Short trials show small median ALT/AST changes; case reports of liver injury exist with unregulated SARM products, quality matters.
CV: No outcomes data; atherogenic lipid shifts warrant caution.
Dermatologic: Mild acne/oiliness; hair shedding in predisposed users.
Hematologic: Mild ↑ hematocrit; monitor if baseline high.
Neuropsych: Irritability, insomnia occasionally reported.
Drug interactions: Potential with agents affecting hepatic enzymes/lipids; avoid pregnancy exposure.

Comparative safety matrix

Concern	Enobosarm (MK-2866)	LGD-4033	Testosterone
Route & t½	Oral; ~24 h	Oral; 24–36 h	IM/SC/TD
Lean-mass gain (short term)	Yes (~1–1.5 kg/12 wks)	Yes (~0.6–1.5 kg/3 wks)	Yes (dose-dependent)
HPG suppression	Moderate	Moderate	Marked (exogenous)
HDL reduction	Common	Common	Variable
Prostate/PSA	Low change short-term	Low	↑ possible
Hepatotoxicity signal	Case reports (unregulated)	Case reports	Low (non-17-α oral)

7. Regulatory Landscape

Approvals: None for any indication.
Enforcement: Regulatory agencies have issued warnings about SARM-containing “supplements” and adulteration.
Sport: WADA-prohibited (S1 Anabolic Agents); strict liability applies.

8. Future Directions

Definitive RCTs in sarcopenia/rehabilitation, powered for function (SPPB, stair-power) and falls/fractures.
Oncology programs in AR-positive ER⁺ breast cancer (rational combinations with CDK4/6 inhibitors and endocrine therapy).
Bone-focused studies (DXA plus microarchitecture/strength metrics).
Safety program: Long-term lipid/CV, hepatic, endocrine recovery tracking with GMP drug supply.
Medicinal chemistry: Next-gen SARMs targeting lipid neutrality and reduced HPG suppression while preserving anabolism.

Selected References

Journal of Clinical Endocrinology & Metabolism; Journal of Cachexia, Sarcopenia and Muscle, Phase 2 human trials of enobosarm on lean mass and function.
FASEB Journal; American Journal of Physiology–Endocrinology, Anti-catabolic signaling and atrogene suppression with SARMs.
Journal of Bone and Mineral Research; Bone, SARM effects on BMD and bone strength in osteopenia models.
The Oncologist; Cancer Research; Annals of Oncology, Enobosarm in cancer cachexia and AR-positive ER⁺ breast cancer strategies.
Clinical Pharmacology & Therapeutics, Oral PK/PD of non-steroidal SARMs.
Drug Testing & Analysis; WADA Laboratory Reports, Detection of MK-2866 metabolites and anti-doping cases.
Hepatology Communications; J Clin Transl Hepatol, Reports of liver injury with unregulated SARM products

MK2866(Ostarine) 100x10mg

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