ACP-105: What Is Known About This Experimental SARM

Selective androgen receptor modulators (SARMs) have garnered attention for their potential to provide the anabolic benefits of traditional steroids without the associated detrimental side effects. Among these, ACP-105 is a novel compound attracting interest due to its specific property profile and implications in sports.

Overview of ACP-105: A Novel SARM

ACP-105 (CAS: 1048998-11-3) is a non-steroidal SARM under research for muscle mass enhancement and potential therapeutic use in testosterone replacement. Despite its promising benefits, its safety and metabolic profiles require thorough exploration, particularly given its applications in sports [PMID: 40928534].

ACP-105 Pharmacokinetics

A recent study has provided the first comprehensive Absorption, Distribution, Metabolism, and Excretion (ADME) profile for ACP-105, employing an integrative in silico approach. The results revealed:

• Gastrointestinal absorption: High, up to 100%
• Lipophilicity: Moderate, with a LogP range of 3.0-3.52
• Solubility: Low, with a LogS range of -4.1 to -4.4
• Permeability: Caco-2 permeability ranging from 13.6 to 152 × 10⁻⁶ cm/s
• Plasma protein binding: Strong, between 77-99%

Additionally, ACP-105 is predicted to cross the blood-brain barrier and undergoes metabolism primarily via CYP3A4, with six metabolites identified [PMID: 40928534].

Metabolic Pathways and Analysis

The understanding of ACP-105’s metabolism is instrumental in doping control. Another study employed a multivariate data analysis (MVDA) approach to compare in vitro derived metabolites of ACP-105 with human metabolites. Systematic optimization of incubation conditions led to the identification of 18 metabolites in vitro and seven in human urine post-administration. Key metabolites for doping control include monohydroxylated forms [PMID: 37972465].

Toxicology and Safety Concerns

Toxicological evaluations of ACP-105 are crucial, given its recreational use in sports. Predicted toxicological endpoints via in silico methods include:

• Acute toxicity: A comprehensive suite of tests suggested potential risks, though quantification in vivo remains unexamined.
• Genotoxicity (Ames Test) and cardiotoxicity testing illustrated concerns, particularly as hERG inhibitors.
• Organ toxicity assessments: Showed interactions that necessitate caution in usage [PMID: 40064700].

Sports Doping and Metabolite Detection

The use of ACP-105 as a doping agent has led to research on its detection through advanced methods. Techniques like UHPLC-MS/MS are being developed for surveillance to identify SARMs, including ACP-105 in hair samples. This contributes to the applicability of its metabolites in doping control and supports the development of testing protocols for sports integrity [PMID: 34814052].

Studied Regimens

In vitro studies provided detailed metabolic and pharmacokinetic data, yet human administration data remains largely unexplored. This gap underscores the importance of further investigations to ascertain the safety and efficacy of potential therapeutic regimens.

Key Takeaways

ACP-105 continues to be a focal point of research in SARMs due to its potential, yet challenges persist, particularly in safety and toxicity profiles. As its detection and metabolic understanding improve, so does its implication in sports doping. The ongoing studies are crucial for both therapeutic advancements and regulatory oversight in sports.

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