Testolone

Areas of active research — not promised effects

Each tag links to other compounds with research into that goal. Research use only: these are areas of study, not human-use claims.

Related by research scope · open each to compare

RAD-140 has no FDA-approved indication and is not scheduled under the Controlled Substances Act. Marketing or selling it for human use — including as a dietary supplement or performance enhancer — is unlawful under the Federal Food, Drug, and Cosmetic Act. The FDA has issued warning letters to multiple vendors marketing SARMs including RAD-140 for human consumption (late 2025). Ellipses Pharmaceuticals holds investigational new drug (IND) status for RAD-140 (as Vosilasarm/EP0062), and an NCT-registered Phase 1 trial has been conducted in breast cancer patients; however, no approval exists. Research-use-only supply to qualified laboratories occupies a grey area but confers no authorisation for human use.

Transparent blend · bci-1.0 · never paid-placement

Primary name

Testolone

Origin

Synthetic small molecule first characterised by Radius Health and later developed as Vosilasarm (EP0062) by Ellipses Pharmaceuticals. RAD-140 was originally designed to provide anabolic effects on skeletal muscle and bone with reduced androgenic stimulation of reproductive tissues, as a potential alternative to testosterone replacement therapy and a treatment for muscle-wasting conditions. The compound has since been investigated in a Phase 1 clinical trial in women with oestrogen receptor-positive, HER2-negative metastatic breast cancer, exploiting its androgen receptor agonist activity in an oncology context. It has never received regulatory approval for any indication in any jurisdiction.

Registry IDs

PubChem CID

44200882

CAS

1182367-47-0

InChIKey

XMBUPPIEVAFYHO-KPZWWZAWSA-N

DrugBank

DB13939

ChEMBL

CHEMBL1672635

Molecular formula

C20H16ClN5O2

Molar mass

393.8 g/mol

Monoisotopic

393.0992525 Da

InChIKey

XMBUPPIEVAFYHO-KPZWWZAWSA-N

Appearance

White to off-white crystalline powder

Solubility

Poorly soluble in water; soluble in DMSO and organic solvents; oral bioavailabil…

Sequence not available in current seed.

Stability: Stable as dry powder under recommended conditions; degrades under prolonged exposure to light, heat, and moisture. Reconstituted solutions should be used prompt

Vial sizes

null mg

Purity grades

≥98% / ≥99%

Salt forms

Free base (primary)

• GHS hazard class on file
• PPE & spill response
• Disposal guidance
• Not-for-human-consumption posture

How much research exists, and of what maturity — never a verdict on whether it works.

Mechanism of action

• RAD-140 binds the androgen receptor (AR) with high affinity, with preclinical characterisation demonstrating an anabolic-to-androgenic ratio exceeding 90:1 relative to testosterone in standard rodent assay systems
• Its nonsteroidal oxadiazolyl benzonitrile scaffold drives differential cofactor recruitment compared with endogenous androgens, producing robust anabolic gene activation in skeletal muscle and bone while generating only attenuated stimulation of the prostate and accessory sex glands
• Unlike testosterone, RAD-140 does not undergo aromatisation to oestrogen or 5α-reduction to dihydrotestosterone, eliminating those conversion-dependent side-effect pathways
• Preclinical neurobiological studies have also reported neuroprotective activity in models of Alzheimer-relevant neuronal stress, attributing this to AR-mediated activation of pro-survival signalling cascades, though this line of investigation remains at the laboratory stage

Pharmacokinetics (ADME)

Half-life

~44–60 hours (human; Phase 1 breast cancer trial at 100 mg single-dose level)

Clearance

Not formally published; PK samples collected over 144 hours post single dose; dose levels studied: 50, 100, and 150 mg/day orally in a Phase 1 trial

PK–PD note: Terminal half-life supports once-daily oral dosing. Human PK data derive from the first-in-human Phase 1 trial in 22 ER+/HER2− metastatic breast cancer patients (Ellipses Pharmaceuticals; MTD 100 mg/d…

Reading the evidence

• Evidence quality and gaps vary by application — see the cited grades above.
• Indexed-article counts span all evidence tiers, not only completed human trials.
• No first-party human-dosing, efficacy, or benefit claims are made here.

Key reviews & evidence-gap sources

• Vignali et al. 2023 — systematic review of SARM safety in healthy adults (J Xenobiotics) — SARM-class review, not RAD-140-specific: 1,225 titles screened, 33 studies included (15 case reports + 18 clinical trials, N=2,136); RAD-140 among the covered compounds. Reports DILI, tendon rupture, rhabdomyolysis and cardiovascular safety signals across the class.
• Miller et al. 2010/2011 — design, synthesis & preclinical characterization of RAD140 (ACS Med Chem Lett) — Original discovery paper (Radius Health): AR binding affinity, rodent tissue-selectivity, primate dosing. Anchors the mechanism-coverage weighting and the preclinical oral-bioavailability figures (rat F 27–63%, monkey F 65–75%).
• LoRusso et al. 2022 — first-in-human Phase 1 of RAD140 in ER+/HER2− metastatic breast cancer (Clin Breast Cancer 22(1):67-77) — [Verification: cite LoRusso et al., NOT 'Yu et al.' — Z. Yu is a co-author, not first author.] The ONE completed, results-published human trial (NCT03088527): single-arm/open-label/non-randomized Phase 1 dose-escalation, 22 postmenopausal women (21 AR+) with ER+/HER2− metastatic breast cancer, 50/100/150 mg/day; MTD 100 mg/day; elimination half-life ~44.7 h. At the 100 mg/day MTD the investigators reported a 24-week clinical benefit rate of 18.2%, one partial response (in a patient with a baseline ESR1 mutation) and median progression-free survival of 2.3 months. Reported strictly as the trial's own attributed Layer-A oncology finding in a metastatic-breast-cancer population — NOT a benefit/efficacy claim for RUO use.
• Heinze et al. 2026 — RAD140 and cardiac function in aged mice, male-specific IL-6-graded effects (GeroScience) — Preclinical (23-month-old mice, 6-week dosing): higher ejection fraction/stroke volume/cardiac output vs controls, sex-dimorphic and IL-6-graded. Hypothesis-generating; not replicated in humans.
• RAD-140 Drug-Induced Liver Injury (The Ochsner Journal 2022;22(4):361-365) — Single (n=1) case report: a 24-year-old man developed severe cholestatic drug-induced liver injury (peak total bilirubin 38.5 mg/dL) after taking RAD-140 ~5 weeks; DILIN causality 'probable', severity 'severe', resolved after cessation. An individual case report (association, not population incidence).
• SARM-associated liver injury case report (Cureus 2024; PMID 39328701) — Single (n=1) case report: a 29-year-old man developed jaundice with drug-induced liver injury (bilirubin 11.3 mg/dL, ALT 144, AST 92) after ~3 months of a RAD-140-containing SARM product (~20 mg/day); resolved ~6 weeks after discontinuation. Association, not proven causation; not asserted as 'the second' such case.

No registered human trials found for this compound.

Status

No registered trials found

Summary (literature)

In the Phase 1 oncology trial at 50–150 mg/day, the most frequent treatment-emergent adverse events were elevated hepatic enzymes (AST 59.1%, ALT 45.5%, bilirubin 27.3%), vomiting, dehydration, and decreased appetite and weight (approximately 27% each). These signals indicate cli…

WADA status

Prohibited in-competition and out-of-competition under WADA 2026 Prohibited List Section S1.2 (Other Anabolic Agents). RAD-140 (testolone) is explicitly named o…

Dominant research route: Oral (PO) is overwhelmingly the only route studied for RAD140/testolone at every stage — from the original rat/monkey preclinical characterization (oral gavage; Miller et al.) through the one completed human trial (oral capsule, single-arm Phase 1 dose-escalation, NCT03088527) — and it is also the only route the research-market vendor line offers (liquid dropper, often described as taken sublingually, or capsules). Exactly one published preclinical study used subcutaneous injection, and only as a mid-study logistical substitute for a lesioned animal that could no longer be gavaged. No IM, IV, IP, intranasal, or topical study of RAD140 was located this pass — undocumented, not asserted absent.

The dominant, essentially only, route studied at every stage. Preclinical: oral gavage 0.03–30 mg/kg in castrated/intact male rats and cynomolgus monkeys, 0.5% methylcellulose suspension (Miller et al. 2011). Human: a completed first-in-human single-arm Phase 1 dose-escalation (NCT03088527; ClinicalTrials.gov status COMPLETED, primary completion Aug 2020) dosed RAD140 as an oral capsule at 50 mg (n=6) / 100 mg (n=13) / 150 mg (n=3) once daily in 22 postmenopausal women with ER+/HER2− metastatic breast cancer; MTD 100 mg/day. Results published in Clinical Breast Cancer (LoRusso et al. 2022) even though the registry record itself shows hasResults=false.

Bioavailability: [Verification: only the 44.7 h elimination half-life is primary-confirmed for humans (LoRusso 2022 abstract), supporting once-daily dosing.] Additional figures circulating in a vendor research guide — Tmax ~1–4 h, oral bioavailability ~70–80% (which the guide itself attributes to 'mammal models,' i.e. animal/preclinical, NOT human), and a ~60 h half-life (only the upper bound of a vendor FAQ '44.7–60 h' range) — could NOT be confirmed against the paywalled primary full text and are NOT stated as human PK. Preclinical (primary-confirmed, Miller et al.): oral bioavailability F = 27–63% in rats and 65–75% in monkeys — a marked improvement engineered over an earlier back-up compound (F<5% in rats).

RAD-140/testolone is a nonsteroidal small-molecule SARM engineered from first synthesis for oral bioavailability — unlike an injectable peptide, it was never designed around a parenteral route. The completed oncology Phase 1 dosed it orally, and the research-market line mirrors that (oral liquid dropper or capsules). Vendor/community guides commonly describe holding the liquid sublingually before swallowing — an attributed Layer-B product-use convention, not a clinical protocol or dosing recommendation. The 50–150 mg/day oncology-trial doses are clinical-research context only, not a research or human-use recommendation. NOTE: tagged evidenceTier 'human_obs' (not 'human_rct') because the trial is single-arm/open-label/non-randomized — a completed human clinical trial, but not a randomized controlled trial.

Documented in exactly one published preclinical study, and only as a dosing-logistics substitution: gonadectomized male rats received RAD140 (1 mg/kg in 0.5% methylcellulose) by oral gavage for a 2-week lead-in, then — after a kainate lesion made oral gavage impractical — were switched to 1 mg/mL RAD140 in safflower oil by daily SC injection for the remainder of a neuroprotection study (Jayaraman/kainate-lesion rat model, PMC3959610).

Bioavailability: No dedicated SC pharmacokinetic or bioavailability characterization exists — the SC injection was a practical workaround for a lesioned animal that could no longer be gavaged, not a study comparing or quantifying the SC route itself.

The only documented parenteral/injected use of RAD140 identified in the literature this pass, and it is animal-only. No injectable RAD-140 research product was identified among vendor listings — the compound is sold and used exclusively as an oral liquid or capsule.

Animal & human figures are kept visibly separate so studied animal doses are never misread as human guidance.

Sorted A–Z by vendor — never by price

Weekly median $/mg from the live vendor crawl.

Researched storefront prices, bucketed

p25 $0.090 · median $0.140 · p75 $0.150 · 12 researched vendors

Legit, COA-backed band: $0.080–$0.160/mg.

Value rule: don't just buy the cheapest — a price under $3/mg is a red flag. Pair price with COA and independent-test grade.

Estimated cost of research (10 mg)

Vial (best researched price)

$0

Bacteriostatic water (generic estimate)

$6

Syringes / supplies (generic estimate)

$12

What each test proves — general guidance, plus this compound's researched purity data

Purity on the current market (researched)

Reputable US research-chem vendors self-report ≥98–99%+ HPLC purity with an accompanying LC-MS/MS identity check (e.g. Chemyo, Loti Labs, Sports Technology Labs, Pure Rawz — the last naming MZ Biolabs). These are vendor-advertised claims, not an independently aggregated market-wide sample — no Finnrick/Janoshik-style large-N purity aggregate specific to Testolone was found this pass. The one INDEPENDENT compound-identity check located (Jendrzejewska et al. 2025) is a more severe signal than a purity percentage: 0 of 4 Testolone-labeled products purchased online in the Slovak Republic (EU grey market) could be confirmed by combined solid-state methods to actually contain testolone — though n=4 and a non-US sales channel limit how far this generalizes.

Independent labs cited for this compound

No product recall specific to a Testolone/RAD-140 product was found (search window through 2026). As with other unapproved research-chemical drugs sold outside the regulated supply chain, FDA action takes the form of warning letters, import detention, and DOJ criminal referral rather than a Class I/II/III recall — reported honestly as an empty recall result, not invented.

Buyer red-flag checklist

• Sold or marketed with bodybuilding/muscle-growth/strength-enhancement language on a page also claiming 'research use only' — the exact pattern cited in the Dec 2025 FDA warning letters (Titan SARMs, Atomix, Prime Sports Nutrition).
• Labeled or sold as a 'dietary supplement' rather than clearly as a research chemical — the marketing pattern most associated with FDA warning letters and DOJ criminal referral for SARMs.
• No batch-specific/lot-matched COA provided on request.
• COA reports purity only, with no LC-MS/spectroscopic identity confirmation — cannot rule out wrong-compound substitution (the exact failure mode documented for Testolone-labeled products in Jendrzejewska et al. 2025).
• COA report/task ID does not resolve in the testing lab's public database.
• No lot/batch number on the vial matching the COA.
• Price far below the market range for the stated mg amount, consistent with an underfilled or off-spec product.

GMP vs research-grade: the chemistry (SPPS + HPLC + MS) is identical — the difference is the quality system.

Underdosing / mislabeling: No large-N independent testing aggregate specific to Testolone/RAD-140 was found this pass, so 0.48 is a class-wide proxy, not a Testolone-specific measurement: Van Wagoner et al. (JAMA 2017) found only 52% of 44 internet SARM products contained ANY labeled SARM (i.e. ~48% did not), and only 41% matched the labeled amount. [Verification corrected: RAD-140 WAS assayed in that study — three products were labeled RAD-140, of which one was confirmed to contain RAD-140 and two were mislabeled — so the earlier 'RAD-140 not among the assayed compounds' framing is dropped. The per-product RAD-140 table detail is drawn from the paper's full-text results table and is worth a one-time human eTable confirmation before publishing as fact.] A small compound-specific 2025 study (Jendrzejewska et al.) found 0 of 4 Testolone-labeled products confirmed by independent spectroscopy — directionally consistent with (or worse than) the class-wide figure, but n=4 is too small to serve as a prevalence estimate on its own.

• FDA Import Alert 66-41 ('Detention Without Physical Examination of Unapproved New Drugs Promoted in the U.S.') is the general unapproved-new-drug DWPE mechanism under which RAD-140/Testolone sold as a research chemical can be detained — but it operates via a firm/product-specific Red List (DWPE applies to marketers/products FDA places on the alert), not a categorical detention of the Testolone molecule, and the alert does not name RAD-140 by compound. An RUO or 'not for human consumption' label is not an import exemption — CBP/FDA judge actual intended use, and the muscle-growth/strength marketing cited in the Dec-2025 warning letters is exactly the pattern that defeats an RUO defense. No SARM-specific import-alert number distinct from this general category was confirmed this pass.66-41 (unapproved new drugs)
• An RUO label is not an import exemption — CBP judges actual intended use.
• Lyophilized powder is ambient-stable in transit; temperature control needed for > 7-day transit.
• US-warehouse vendors dodge import scrutiny — they cost more but ship more reliably.

Every item dated & sourced

Prohibited AT ALL TIMES (in- and out-of-competition) under the WADA 2026 Prohibited List, category S1.2 'Other Anabolic Agents' — a non-Specified Substance (the strictest sanction tier). The 2026 List names RAD140 explicitly as an example SARM in S1.2, alongside andarine, enobosarm (ostarine), LGD-4033 (ligandrol), S-23 and YK-11. No FDA-approved human therapeutic use exists for RAD-140 in the bodybuilding/supplement context, so there is no Therapeutic Use Exemption pathway; anti-doping bodies treat a RAD-140 positive the same as an anabolic-agent violation. [Verified against the WADA 2026 Prohibited List PDF (in force 1 Jan 2026); USADA is the corroborating secondary source.]

No granted patents identified in current seed. Composition-of-matter coverage is limited given the peptide's synthetic origin.

• IACUC / IRB research context
• RUO buyer responsibilities & documentation
• Veterinary / alternative-use where lawful
• Jurisdiction-aware "who may lawfully obtain"

What people discuss

Reported concerns — discussion, not established effects

Reading caveats

• Survivorship / bro-science positivity bias — dramatic before/after transformation posts over-shared relative to null or negative cycles
• SEO / AI-generated 'best SARM' and vendor-run blog content crowds out genuine peer-forum discussion in any automated discourse read
• Affiliate / discount-code incentive embedded in YouTube reviews and vendor 'where to buy' round-ups
• Anecdotal self-report bias — concurrent compound use, dosing, diet and training are rarely disclosed or controlled
• Negativity bias in adverse-event / liver-concern threads relative to the much larger, less-visible pool of uneventful cycles
• Case-report visibility bias — a handful of published clinical liver-injury case reports (see evidence keyReviews) may be over-referenced in discussion relative to true incidence

Manually researched from reddit, youtube— theme weights are research estimates, not live counts; aggregated & de-identified. No individual posts, quotes, or usernames are ever shown.

Relative research / market volume — populated once the activity stream is wired

Inline tooltips for lyophilized, RUO, EU/mg, SPPS, 503A and more.

Toggle plain-language ↔ scientific in the header.

• How to read a COA
• Free base vs acetate
• Understanding evidence grades

Oral nonsteroidal SARM (RAD-140) with high AR affinity; under clinical investigation for breast cancer; not approved; prohibited in sport. Approximately 6 articles are indexed (literature last scanned 2026-05-29). US regulatory status: Not FDA-approved; not a scheduled controlled substance; RUO only. Research use only.

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