Anastrozole 0.1mg | Clomiphene 20mg | DHEA 20mg | 7-Keto DHEA 20mg | Pregnenolone 20mg
Anastrozole 0.1mg | Clomiphene 20mg | DHEA 20mg | 7-Keto DHEA 20mg | Pregnenolone 20mg is part of a prescriber-directed hormone or endocrine protocol. It should be selected based on symptoms, diagnosis, labs when appropriate, route preference, contraindications, and ongoing monitoring.
This is a multi-ingredient compounded oral capsule containing Anastrozole 0.1 mg, Clomiphene 20 mg, DHEA 20 mg, 7-Keto DHEA 20 mg, and Pregnenolone 20 mg, prepared by Genesis Compounding as a patient-specific, prescriber-directed 503A preparation. This formulation is designed to support endogenous testosterone production and hormonal precursor availability in men with secondary hypogonadism, combining an aromatase inhibitor (anastrozole), a SERM (clomiphene), and adrenal/neurosteroid precursors (DHEA, 7-Keto DHEA, pregnenolone). This preparation is not FDA-approved as a compounded preparation.
| Active Ingredient | Pharmacologic Role |
|---|---|
| Anastrozole 0.1 mg | Non-steroidal aromatase inhibitor (AI) that blocks CYP19A1-mediated conversion of androgens to estrogens, reducing estrogenic negative feedback on the hypothalamic-pituitary axis and thereby supporting endogenous LH and testosterone production. |
| Clomiphene 20 mg | Selective estrogen receptor modulator (SERM) that competitively blocks estrogen receptors at the hypothalamus and pituitary, reducing estrogen-mediated negative feedback and increasing pulsatile GnRH, LH, and FSH secretion to stimulate testicular testosterone and sperm production. |
| DHEA 20 mg | Adrenal androgen precursor hormone that is peripherally converted to testosterone and estradiol by tissue-specific steroidogenic enzymes, supporting androgen availability without directly suppressing the hypothalamic-pituitary-gonadal (HPG) axis. |
| 7-Keto DHEA 20 mg | Non-androgenic metabolite of DHEA that does not convert to testosterone or estrogens; supports thermogenic metabolism via upregulation of mitochondrial enzymes and may modulate cortisol activity; included for metabolic support without further androgenic contribution. |
| Pregnenolone 20 mg | The primary steroidogenic precursor synthesized from cholesterol, serving as the substrate for all downstream steroid hormones (progesterone, DHEA, cortisol, testosterone, estrogens); also acts as a neurosteroid modulating GABA-A and NMDA receptor activity. |
Administered orally as a capsule.
- Typically taken once daily with or without food, as directed by the prescriber.
- Swallow whole with water.
- Consistent daily dosing at the same time supports stable hormone levels.
This multi-component capsule contains sub-therapeutic doses of each ingredient designed for hormonal axis support rather than full-dose pharmacologic treatment. Key dosing principles:
- Anastrozole: at 0.1 mg, this is a low-dose AI, well below the 1 mg oncologic dose, intended to modestly reduce estrogen-mediated HPG feedback without significant estrogen suppression below physiologic range.
- Clomiphene: 20 mg is a low initiation dose; standard clinical doses in male hypogonadism range from 25–50 mg daily or three-times-weekly.
- DHEA/7-Keto DHEA/Pregnenolone: 20 mg each are within supplemental ranges.
- All dosing is prescriber-determined based on serum testosterone, LH, FSH, estradiol, and clinical response. Titration may be required.
- Anastrozole: Competitively and selectively inhibits CYP19A1 (aromatase), the enzyme responsible for converting androstenedione and testosterone to estrone and estradiol. Reduced estrogen reduces negative estrogenic feedback on the hypothalamus and pituitary, increasing GnRH and LH/FSH pulse amplitude and stimulating testicular Leydig cell testosterone synthesis.
- Clomiphene: Acts as an antagonist at hypothalamic and pituitary estrogen receptors (ERα), blocking the inhibitory estrogenic feedback signal. The resulting increase in GnRH release drives increased LH and FSH secretion from the anterior pituitary, stimulating Leydig cells (testosterone) and Sertoli cells (spermatogenesis) in the testes without suppressing the HPG axis.
- DHEA: Undergoes peripheral conversion to testosterone via 17β-hydroxysteroid dehydrogenase and to estrogens via aromatase in adipose, skin, liver, and other tissues, providing androgen substrate without HPG axis suppression.
- 7-Keto DHEA: A 7-oxygenated DHEA metabolite that does not interconvert to DHEA or sex hormones; activates thermogenic enzymes (mitochondrial glycerol-3-phosphate dehydrogenase, cytosolic malic enzyme) and may inhibit 11β-HSD1 (reducing local cortisol activation), supporting metabolic function.
- Pregnenolone: Synthesized from cholesterol in mitochondria, pregnenolone is the universal steroidogenic precursor and is converted to progesterone, DHEA, 17-hydroxypregnenolone, and downstream sex and adrenal steroids depending on tissue-specific enzyme expression; additionally modulates GABA-A and NMDA receptor function as a neurosteroid.
This combination preparation is used in the prescriber-directed management of male secondary (hypogonadotropic) hypogonadism and fertility-preserving testosterone support:
- Clomiphene and anastrozole both increase endogenous testosterone through HPG axis mechanisms, preserving intratesticular testosterone and spermatogenesis — critical advantages over exogenous testosterone replacement in men who wish to maintain fertility.
- DHEA and pregnenolone provide precursor substrate support for endogenous steroidogenesis.
- 7-Keto DHEA contributes metabolic support without androgenic or estrogenic effects.
Monitoring:
- Serum total and free testosterone, LH, FSH, estradiol, SHBG, and DHEA-S at baseline and 4–6 weeks after initiation, then every 3 months.
- Semen analysis for men seeking fertility preservation.
- Hematocrit (elevated erythropoiesis risk at higher testosterone levels), liver function, and lipid panel annually.
- Monitor estradiol: anastrozole at 0.1 mg should prevent excess estrogen, but over-suppression (estradiol <20 pg/mL) can impair libido, bone, and lipid profiles.
Contraindications:
- Hypersensitivity to anastrozole, clomiphene, or any component.
- Liver disease (clomiphene and anastrozole are hepatically metabolized).
- Hormone-sensitive malignancy (androgen-sensitive prostate cancer — testosterone stimulation risk).
Warnings & Precautions:
- Clomiphene (zuclomiphene isomer) has a prolonged half-life and may accumulate with daily dosing.
- Anastrozole at low doses should prevent estrogen over-suppression, but clinicians should monitor estradiol closely.
- DHEA in high doses may promote androgenic side effects (acne, hair loss) and, theoretically, hormone-sensitive tumor growth — use under medical supervision.
- Pregnenolone may affect adrenal feedback loops; monitor for adrenal-related symptoms.
Drug Interactions:
- Anastrozole: CYP3A4 interactions are possible; tamoxifen co-administration reduces anastrozole plasma levels.
- Clomiphene: avoid concomitant use with danazol; hepatotoxic drugs should be avoided.
- DHEA: may reduce the effectiveness of antidiabetic drugs; interacts with SSRIs and triazolam.
Common Side Effects: Hot flushes (clomiphene), acne, oily skin (androgen excess from DHEA), joint pain or stiffness (anastrozole at higher doses), mood changes, visual disturbances (rare — clomiphene).
Store at room temperature (15–25°C), protected from heat and moisture. Keep in a cool, dry location. Keep out of reach of children. Observe the beyond-use date assigned by Genesis Compounding per USP <795>.
How does this preparation increase testosterone without testosterone replacement?
Both clomiphene (by blocking estrogen feedback at the pituitary) and anastrozole (by reducing estrogen synthesis) stimulate the pituitary to release more LH and FSH, which in turn signal the testes to produce more testosterone naturally. This preserves fertility and the normal HPG axis, unlike exogenous testosterone.
Why are DHEA and pregnenolone included?
DHEA is a natural androgen precursor that provides additional substrate for testosterone synthesis in peripheral tissues. Pregnenolone is the master steroid precursor supporting overall adrenal and gonadal steroidogenesis. Both are included to broadly support hormonal balance alongside the axis-stimulating agents.
What is 7-Keto DHEA and why is it different from regular DHEA?
7-Keto DHEA is a metabolite of DHEA that does not convert to testosterone or estrogens. It is included primarily for its metabolic (thermogenic) properties and does not add androgenic burden to the formulation.
Is this preparation FDA-approved?
No. This is a patient-specific, 503A compounded preparation from Genesis Compounding. While anastrozole and clomiphene are FDA-approved for other indications, this specific multi-ingredient combination is compounded to order per prescriber direction.
What labs should be monitored?
Your prescriber will check testosterone (total and free), LH, FSH, estradiol, SHBG, and DHEA-S at baseline and follow-up visits. Monitoring estradiol is particularly important to ensure the anastrozole component is not suppressing estrogen below the physiologic range.
Clinical References
Authoritative sources reviewed in preparing this clinical summary. Provided for prescriber reference; not a substitute for the prescriber’s clinical judgment.