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Rad3.2

RAD-140 (Testolone) – Forschung

Überwiegend Mechanismus / Beobachtung

6 begutachtete Studien

Was die Evidenz sagt

Überwiegend Mechanismus / Beobachtung

Die meisten Studien zu RAD-140 (Testolone) sind mechanistisch oder beobachtend statt RCTs, die einen klinischen Effekt messen — betrachte die Ergebnisse als vorläufig.

Die meiste Evidenz stammt aus gemischt-qualitativen Studien, veröffentlicht 2011–2024 mit einer typischen Studiengröße von 22 Teilnehmenden.

Basierend auf 6 Studien · 22 Teilnehmende insgesamt

Konfidenz

Geringe Konfidenz

Nach Outcome

Muscle & body composition (preclinical)Anabole/körperzusammensetzungsbezogene Effekte sind präklinisch; keine kontrollierten Studien am Menschen zum Muskelaufbau. Birgt das Risiko von Leberschäden und Testosteronsuppression. · Nicht belegt (keine Wirksamkeitsstudien am Menschen)
Überwiegend Mechanismus / Beobachtung6 Studien
Androgen & hormonal axis
Überwiegend Mechanismus / Beobachtung6 Studien
Liver injury
Zu wenige bewertete Studien2 Studien
Safety profile
Zu wenige bewertete Studien2 Studien

Aktives Forschungsgebiet

4 Studien in den letzten 5 Jahren

201120172024

1Safety, tolerability, MTD, and pharmacokineticsOpen-Labeln=22 · very small study2022

RAD140 is a novel oral AR-targeted agent with an acceptable safety profile and preliminary evidence of target engagement and antitumor activity; the most frequent treatment-emergent adverse events were elevated AST (59.1%) and ALT (45.5%).

LoRusso, Hamilton, Ma, Vidula, Bagley, Troy · Clinical breast cancer (2022)

First-in-human Phase-1 dose-escalation (3+3) — a safety/PK study, not an efficacy RCT
22 heavily pretreated ER+/HER2- metastatic breast-cancer patients; 50–150 mg/day
Liver-enzyme elevations (AST 59.1%, ALT 45.5%) were the most common adverse events

Quelle ansehen

2Beobachtungsstudie2024

In 23% of samples, the expected SARM was not detected but a different one instead ... Other undeclared pharmaceutical substances (tamoxifen, clomifene, testosterone, epimethandienone, tadalafil) were measured in 30% of samples.

Gaudiano MC, Aureli F, Manna L, Borioni A, Maccelli A, Raimondo M, et al. · Sexual medicine (2024)

Recent (2024) analytical study of 13 SARM products purchased online — reinforces the mislabeling/contamination finding
Qualitative analysis confirmed the stated SARM in only ~70% of samples; 23% contained a different SARM and one contained none; content ranged 30-90% of label claim
30% of products contained undeclared drugs (tamoxifen, clomifene, testosterone, tadalafil) and >60% contained more than one active substance

Quelle ansehen

3Präklinisch2011

This report describes the discovery of RAD140, a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM), characterized in several preclinical models of anabolic androgen action.

Miller, Shomali, Lyttle, O'Dea, Herendeen, Gallacher · ACS medicinal chemistry letters (2011)

Foundational discovery paper for RAD-140 from Radius Health
Characterized RAD-140 as a potent, orally bioavailable nonsteroidal SARM
Anabolic androgen activity demonstrated only in preclinical models

Quelle ansehen

4AR/ER+ breast-cancer xenograft growth inhibitionIn vitro2017

RAD140 is a potent AR agonist in breast cancer cells that inhibits the growth of multiple AR/ER+ breast cancer patient-derived xenograft models as a single agent.

Yu, He, Wang, Patel, Miller, Brown · Clinical cancer research (2017)

In-vitro and xenograft (preclinical) study, not a human trial
RAD-140 bound the AR with high affinity and inhibited AR/ER+ breast-cancer growth
Suppressed the ER pathway including the ESR1 gene; effect enhanced with palbociclib

Quelle ansehen

5Fallstudie2024

Severe liver injury following use of RAD-140, a selective androgen receptor modulator, for body building.

Perananthan, George · Australian prescriber (2024)

Human case report of severe liver injury attributed to RAD-140 used for bodybuilding
Direct human harm signal from grey-market body-composition use
Reinforces the drug-induced liver injury pattern seen across SARM case reports

Quelle ansehen

6Fallstudie2023

A 22-year-old previously healthy male who took the SARM RAD-140 for 16 weeks developed jaundice and cholestatic liver injury; liver biopsy showed a picture consistent with drug-induced liver injury.

Mohamed, Jahagirdar, Fatima, Ahmed, Jaber, Wang · Cureus (2023)

Human case report: 22-year-old man took RAD-140 for 16 weeks
Presented with jaundice, markedly elevated bilirubin, and cholestatic liver injury
Biopsy consistent with drug-induced liver injury; enzymes normalized 3–12 months after stopping

Quelle ansehen

In der Forschungsbibliothek ansehen

RAD-140 (Testolone) – Forschung

Überwiegend Mechanismus / Beobachtung

A First-in-Human Phase 1 Study of a Novel Selective Androgen Receptor Modulator (SARM), RAD140, in ER+/HER2- Metastatic Breast Cancer.

Illegal products containing selective androgen receptor modulators purchased online from Italy: health risks for consumers.

Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140.

Selective Androgen Receptor Modulator RAD140 Inhibits the Growth of Androgen/Estrogen Receptor-Positive Breast Cancer Models with a Distinct Mechanism of Action.

Severe liver injury following use of RAD-140, a selective androgen receptor modulator, for body building.

Selective Androgen Receptor Modulators (SARMs)-Induced Liver Injury: A Case Report and Review of Literature.