Cardarine (GW-501516) 10 mg

🔬 Key Studies on Cardarine (GW‑501516)

1. Phase II Dyslipidemia Trial in Humans

Title: GW501516 in subjects with low HDL-cholesterol (Phase II, GlaxoSmithKline)

• A multicenter, randomized, double‑blind, placebo‑controlled dose-range study (12 weeks) investigating 2.5, 5.0, and 10 mg daily in adults with HDL‑C ≤45 mg/dL.

• Results: up to 17% increase in HDL‑C, 7–15% reduction in LDL and triglycerides, improved lipoprotein subclass profiles (e.g., fewer small LDL, increased HDL particles) Clinical Trials Register+10BEHEMOTH LABZ+10Therapeutic Goods Administration (TGA)+10Wikipedia+7PubMed+7ClinConnect+7.

2. Exploratory Lipoprotein Particle Substudy

Title: Lipoprotein subclass profiling with GW501516

• A small exploratory arm (n≈37) escalated from 5 mg to 10 mg daily.

• Findings: significant reductions in very‑LDL (~19%), intermediate LDL (~52%), small LDL (~14%), and increases in HDL particle number (~10%) PubMed.

3. Phase I / Phase II Early Safety Trials

Title: Safety and tolerability of daily GW501516 dosing in healthy volunteers

• Phase I/II trials (2000–2007) assessed 2.5–10 mg once daily for up to 12 weeks in sedentary adults.

• No significant adverse impact on liver or muscle enzymes. Triglycerides improved, and HDL rose modestly, with no acute safety signals noted Reddit.

4. Preclinical Animal Studies & Mechanistic Research

Title: Effects of GW501516 on endurance, metabolism, and cancer risk

• In mice and obese non‑human primates, Cardarine significantly enhanced endurance performance, fatty acid oxidation, and HDL elevation; but long-term studies revealed carcinogenicity in multiple organs, prompting drug development termination in 2007 Reddit+10Wikipedia+10biolongevitysupplements.com+10.

• Animal models established changes in gene expression associated with mitochondrial biogenesis, anti-inflammatory cytokines, and energy metabolism via PPARδ activation biolongevitysupplements.com.

⚠️ Research & Medical Context

• Originally developed for treating metabolic syndrome, obesity, dyslipidemia, and cardiovascular conditions—clinical development reached Phase II but was terminated due to long-term carcinogenicity in animals Clinical Trials RegisterPubMedHealth+1Reddit+1Wikipedia+1PubMed+1CDEK+1MedPath+1PubMed+7The Conversation+7BEHEMOTH LABZ+7BEHEMOTH LABZ+3The New Yorker+3Therapeutic Goods Administration (TGA)+3.

• Mechanism: Selective PPARδ agonist that enhances fatty acid oxidation, HDL production, and mitochondrial function via transcriptional activation in skeletal muscle and liver tissues Wikipedia+10Reddit+10biolongevitysupplements.com+10.

• Safety concerns: Chronic rodent exposure at high doses caused tumors in multiple tissues, including liver, bladder, stomach; human trials showed no acute signals, but were short-term and did not assess carcinogenicity risks WikipediaThe Conversationbiolongevitysupplements.com.

• Regulatory status: Not FDA approved. Added to WADA’s prohibited list in 2009 due to misuse in sports and health risks Wikipedia+1biolongevitysupplements.com+1.