This document discusses oral drug treatments for uterine fibroids. It outlines that selective progesterone receptor modulators (SPRMs) like ulipristal acetate and mifepristone are promising drugs that can reduce fibroid volume. Orally active gonadotropin-releasing hormone (GnRH) antagonists like elagolix are in phase III trials. Selective estrogen receptor modulators (SERMs) and aromatase inhibitors are less effective. Non-hormonal treatments including vitamin D, curcumin, and green tea extract may play a preventative role. SPRMs require intermittent dosing to avoid endometrial thickening and changes, and it is better to begin with GnRH agonists before

1. ORAL DRUGS FOR
TREATMENT OF
MYOMA
By
Magdy abdelrahman mohamed
Assistant prof. of OB/GYN
Sohag university

2. WHY MEDICAL TTT
High rate of recurrence.
Adjunct to surgery.
Complication of surgery
even minimally invasive.
More accepted by patients.
Suitable for patients near
menopause.

3. WHY ORAL MEDICATION
More convenient.
 Avoidance of injection site
reactions.
More economic.
Could be used daily for long time.

4. IDEAL MEDICATIONS
Curative rather than suppressive
Long-term use should be safe and affordable
Non-contraceptive nature
Not teratogenic.
Inhibits the growth of already existing lesions
Aborts the development of new lesions.
Acceptable side effect
Bedaiwy M et al, Fertil Steril 2017

5. TREATMENT OF MYOMA
Surgical ( myomectomy,
Hysterectomy)
Nonsurgical conservative
interventions.
Uterine artery embolization.
Focused energy.
Radio frequency myolysis.
Medical .
Vilos GA et al, 2015.

7. ORAL DRUGS FOR FIBROID
Promising Drugs:
Selective progesterone receptor modulator
(SPRM). Ex. Ulipristal acetate.
Orally active GnRH antagonists (Elagolix).
Less effective Drugs:
Selective estrogen receptor modulators (SERM)
Aromatase inhibitor.
Vitamin D, curcumin & green tea extract.

8. SELECTIVE PROGESTERONE
RECEPTOR MODULATOR (SPRM)
Ulipristal acetate
(UPA).
Mifepristone.
Asoprisnil.
Telapristone
acetate.
Vilaprisan.

9. ULIPRISTAL ACETATE (UPA)
Inhibits the proliferation of cultured
myoma cells & Induction of
apoptosis.
Only SPRMs approved as medical
therapy of myoma in Europe and
Canada.
35% reduction in myoma volume
after 3 months of UPA treatment.
Reports of rare serious liver injury,
4 cases required transplantation.
Donnez J et al, Fert. Steril 2016.

10. MIFEPRESTONE
Dose 5-10 mg/day.
 A meta analysis by Shen Q et al, 2013, It is
effective in reducing myoma volume,
hypermenorrhea, pelvic pain, anemia, and
dysmenorrhea.
The fact that mifepristone in has been
use for medical abortion for long time
……↑ safety .

11. ASOPRISNIL (ASP)
In 2005, clinical trials with ASP were
suspended by the manufacturer due to
abnormal findings in endometrial biopsies
of treated women.
Williams AR et al, Hum Reprod. 2007.

12. SPRM & ENDOMETRIAL
CHANGES
Unopposed estrogenic stimulation for long
period.
Thickened endometrium
Histological changes (mostly reversible)
Intermittent course preferred.
Better to begin with GNRH then SPRM.
Farris M et al, 2019

13.  Donnez et al. ( 2016).

14. ORALLY ACTIVE GNRH
ANTAGONISTS
Elagolix
Nonpeptidic, orally active.
50–200 mg/day. …rapid supppression.
Significantly reduce heavy menstrual
bleeding.
Still in phase III trial as regard ttt of myoma.
SKI-2670, SKI-2496 & Relugolix (TAK-385):
 other oral antagonist still in animal phase of study.
 (Archer DF et al, 2017)

15. SELECTIVE ESTROGEN RECEPTOR
MODULATORS (SERM)
The primary roles of estrogen in myoma
growth are permissive, in that they enable
tissue to respond to progesterone by
inducing the expression of PR.
The effect of raloxifene on myoma size
and bleeding patterns is unclear .
 (Deng L et al, 2012)

16. AROMATASE INHIBITOR (AIS)
A Cochrane review by Song et al. 2013, no
significant data which would support a wider
clinical use of AIs in myoma-related bleeding.
Better results of AIs in African-American
populations than white races
(Kashani et al, 2016)

17. NON HORMONAL TREATMENT
Vitamin D, curcumin & green tea extract.
A vitamin D deficiency as a risk factor for
the development of myomas.
May have role in prevention & decrease
growth of myoma.
 Ciebiera M et al, 2017