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Injectable Estradiol Formulations Available for Transfeminine People in the United States

By Aly W. | First published June 3, 2020 | Last modified April 27, 2021

Preface

This page is up-to-date as of June 2020. It is likely to become outdated with time.

Introduction

Injectable estradiol is available for transgender people in the United States largely in the forms of oil solutions of estradiol cypionate (brand name Depo-Estradiol) and estradiol valerate (brand name Delestrogen plus generics). These compounds are estradiol esters and are prodrugs of estradiol that are converted into estradiol in the body. They are administered by intramuscular or subcutaneous injection and have a depot effect providing an extended duration of action.

Injectable estradiol is available for people in the United States domestically in pharmaceutical formulations from conventional pharmacies and in compounded formulations from compounding pharmacies. Injectable estradiol is also available internationally from online pharmacies (generally without a prescription) and from certain online members of our community in unregulated homebrewed formulations (also without a prescription of course).

Pharmaceutical Formulations

The only pharmaceutical formulations of injectable estradiol marketed in the United States are oil solutions of estradiol cypionate and estradiol valerate. They include the following (Drugs@FDA):

  • Depo-Estradiol (estradiol cypionate 5 mg/mL in oil) by Pharmacia & Upjohn (FDA)
    • Average $155 (or $130 w/ coupon) for one 5-mL 5 mg/mL (25 mg total) vial (GoodRx)
      • Works out to $135 (or $113 w/ coupon) per month for a dosage of 5 mg/week
  • Delestrogen (estradiol valerate 10, 20, and 40 mg/mL in oil) by Par Sterile Products (FDA)
    • Average $180 (or $140 w/ coupon) for one 5-mL 10 mg/mL (50 mg total) vial (GoodRx)
      • Works out to $78 (or $61 w/ coupon) per month for a dosage of 5 mg/week
    • Average $230 (or $200 w/ coupon) for one 5-mL 20 mg/mL (100 mg total) vial (GoodRx)
      • Works out to $50 (or $44 w/ coupon) per month for a dosage of 5 mg/week
    • Average $400 (or $315 w/ coupon) for one 5-mL 40 mg/mL (200 mg total) vial (GoodRx)
      • Works out to $44 (or $34 w/ coupon) per month for a dosage of 5 mg/week
  • Generics of estradiol valerate 10, 20, and 40 mg/mL in oil by American Regent (FDA) and Hikma Pharmaceuticals (FDA)
    • No prices found for 5-mL 10 mg/mL (50 mg total) vial (GoodRx)
    • Average $140 (or $45 w/ coupon) for one 5-mL 20 mg/mL (100 mg total) vial (GoodRx)
      • Works out to $30 (or $10 w/ coupon) per month for a dosage of 5 mg/week
    • Average $215 (or $65 w/ coupon) for one 5-mL 40 mg/mL (200 mg total) vial (GoodRx)
      • Works out to $23 (or $7 w/ coupon) per month for a dosage of 5 mg/week

Brand-name formulations (i.e., Depo-Estradiol and Delestrogen) are identical to generic formulations and hence the generics, which are less expensive, should be preferred where available. Although generics of estradiol valerate are available, unfortunately no generic formulations of the longer-lasting (and hence more convenient) estradiol cypionate remain marketed.

There have been recurrent problems with shortages of pharmaceutical formulations of injectable estradiol valerate in the United States (The Guardian/Redden, 2016; TAG, 2016; The Philadelphia Inquirer/Friedman-Rudovsky, 2016; Geffen et al., 2018; Vice/Blum, 2018; RPR/Krohn, 2019).

Compounded Formulations

Injectable estradiol valerate in oil can be obtained quite inexpensively from certain accredited compounding pharmacies in the United States (MGS). Many transfeminine people in the United States get their estradiol valerate in this way. Examples of compounding pharmacies that stock estradiol valerate include AnazaoHealth in Las Vegas, Nevada and New Era Pharmacy in Portland, Oregon (MGS). Other compounding pharmacies may also stock injectable estradiol formulations. Compounding pharmacies are often useful avenues during pharmaceutical estradiol valerate shortages. It should be noted that while perfectly legal, compounded medications are not subject to the same regulations and standards as pharmaceutical medications and hence their quality is not guaranteed in the same way that pharmaceuticals are.

International Sources

Pharmaceutical Formulations

Pharmaceutical injectable estradiol is also available in the United States via internationally-shipping online pharmacies located outside of the United States. See the r/TransDIY Wiki for a list of pharmacies.

Homebrewed Formulations

Unregulated homebrewed formulations of injectable estradiol—compounded by certain transfeminine people—are sold online inexpensively by Lena in Kiev, Ukraine and by Lilian of “Otokonoko Pharmaceuticals” in Brazil (Aly W., 2019). They both ship internationally, including to the United States. These homebrewed products are created from powders presumably obtained from sources like online Chinese chemical sellers. Online homebrewers have not only estradiol valerate but also the longer-acting estradiol enanthate (Aly W., 2019) and other estradiol esters. It should be cautioned that these preparations are not subject to regulations and their quality, efficacy, and safety are not guaranteed.

Other Formulations

Estradiol benzoate in oil is a shorter-acting estradiol ester that may remain available from certain online pharmacies. Other estradiol esters such as the long-acting estradiol undecylate (in oil) and polyestradiol phosphate (in water) have been discontinued and are no longer available from any source. Microcrystalline aqueous suspensions of estradiol esters, which have longer durations than oil solutions but also entail more painful injections, were previously sold by certain online pharmacies but likewise appear to no longer be available for people in the United States (Aly W., 2019).

Dosage

See my articles here and here for recommended dosages of injectable estradiol. The TL;DR is that regardless of ester, the dosage may range from 1 to 10 mg/week total depending on the person’s intentions for therapy and the desired estradiol levels (ranging from low-physiological levels or about 50 pg/mL on average to highly supraphysiological levels or about 500 pg/mL on average). An optimal dosage for estradiol monotherapy in terms of efficacy and safety is 5 mg/week total. This is anticipated to provide roughly 90% suppression of testosterone levels, to around 50 ng/dL typically (Wiki; Wiki-Graphs). However, free and hence bioactive testosterone levels will be proportionally lower and further into the female range than total estradiol levels due to estradiol-mediated elevation in sex hormone-binding globulin (SHBG) production and levels (Deutsch et al., 2015). The 5 mg/week total dosage can be delivered as 3.5 mg every 5 days or 5 mg every 7 days for estradiol valerate, 5 mg every 7 days for estradiol cypionate, or 10 mg every 14 days for estradiol enanthate. Note that different estradiol esters have essentially equivalent estrogenic potency (i.e., strength) (Aly W., 2018).

See also here for published time–concentration curves of estradiol levels with injectable estradiol esters and here for approximate durations of estradiol esters with different single-injection doses.