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Hormone regimens for adult transgender persons

	Dose range	Comment
Transfeminine regimens (MTF transgender persons)*
Estrogen^¶
Oral: estradiol (17-beta-estradiol valerate)	2 to 4 mg/day	Some providers report giving higher doses.
Transdermal: estradiol patch	0.025 to 0.2 mg per 24 hours, changed once or twice weekly, depending on specific preparation type	Lower risk of thromboembolism compared with oral estrogen options.
Parenteral
Estradiol valerate	5 to 30 mg IM every two weeks	Prolonged time to onset of effect and steady state, greater risk of accumulation and overdose.
Estradiol cypionate	2 to 10 mg IM every week
Antiandrogens*
Spironolactone	100 to 300 mg/day oral	Monitor blood pressure and electrolytes.
Cyproterone acetate^Δ	25 to 50 mg/day oral
GnRH agonists
Leuprolide	3.75 to 7.5 mg IM depot monthly OR 11.25 mg IM depot every 3 months	Inhibits gonadotropin secretion.
Goserelin	3.6 mg SQ implant monthly	Expensive.
Transmasculine regimens (FTM transgender persons)
Testosterone^◊
Parenteral
Testosterone enanthate or cypionate	50 to 100 mg IM or SQ every week OR 100 to 200 mg IM every two weeks	Weekly injections produce less peak-trough variation in effect (eg, mood); injection site reaction may occur.
Testosterone undecanoate^Δ^§	1000 mg IM every 10 to 12 weeks	Produces stable physiologic testosterone levels over 10 to 13 weeks.
Transdermal
Testosterone gel 1% and 1.6%	5 to 10 grams of gel per day (equivalent to 50 to 100 mg/day testosterone)	Less variation in serum testosterone levels than injectable preparations; gel formulations can result in interpersonal transfer if contact occurs before fully dried (rare).
Testosterone patch	2.5 to 7.5 mg/day transdermal	Transdermal patch may produce lower serum testosterone levels and more skin irritation compared with gels.

Suggestions shown in table are based upon case descriptions and experience. Regimen and dose must be carefully individualized based upon patient age, goals of therapy, whether pre- or postgonadectomy, and comorbid medical conditions and risks. Refer to UpToDate topics on transgender men and transgender females.

MTF: male-to-female; IM: intramuscular; GnRH: gonadotropin-releasing hormone; SQ: subcutaneous; FTM: female-to-male.
* Dose of estrogen should be adjusted according to serum 17-beta-estradiol levels (ie, 100 to 200 pg/mL) and effect. Lower doses of estradiol are generally sufficient for feminization goals when combined with an antiandrogen, GnRH agonist, or after gonadectomy. Antiandrogen therapy is discontinued after gonadectomy.
¶ Synthetic estrogens (eg, ethinyl estradiol) are not recommended, due to elevated risk of thromboembolic disease, cardiovascular mortality, and inability to regulate dose by measurement of serum levels.
Δ Not available in the United States. Available widely elsewhere.
◊ Doses of testosterone should be adjusted according to serum testosterone levels (ie, normal male range 320 to 1000 ng/dL) and effect. Time to onset of effect of parenteral preparations may be less than with transdermal preparations. Supplemental agents such as depot medroxyprogesterone 150 mg every 3 months or oral medroxyprogesterone 5 to 10 mg/day or oral lynestrenol 5 to 10 mg/day (not available in the United States) have been used as an add-on option when starting testosterone therapy to induce cessation of menses.
§ 1000 mg initially, followed by an injection at 6 weeks, then at 12-week intervals.

Data from:

Hembree WC, Cohen-Kettenis PT, Gooren L, et al. Endocrine treatment of gender-dysphoric/gender-incongruent persons: An Endocrine Society* clinical practice guideline. J Clin Endocrinol Metab 2017; 102:1.

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