Elgozon-elagolix Doctor Presentation (1).pptx

A newer drug in treatment of endometriosis

1. Endometriosis 25 40 190,000,000 Women Aged Between have years 10%

2. Elgozon (Elagolix) is a GnRH receptor antagonist indicated for the management of moderate to severe pain associated with ENDOMETRIOSIS

3. To help relieve moderate to severe pain due to a condition called  endometriosis. Painful/heavy/irregular menstrual periods. Pain during or after sex, or  infertility. Indications

4. Approved by the US FDA on 23 July 2018. In Oct 2018, Approved by Health Canada.

5. tissue that is similar to the inner lining of the uterus grows outside the uterus. A condition In which Endometriosis

6. Estrogen is a hormone produced by your body. During your menstrual cycle, Estrogen levels rise & can cause endometriosis lesions to grow. The lesions can break down & shed, causing pain throughout the month. Estrogen fuels Endometriosis Pain

7. 33% of women with endometriosis do not respond to treatment with oral contraceptives and progestogens. Reference: https://www.mdpi.com/1422-0067/22/21/11342 RESISTANCE TO ORAL CONTRACEPTIVES AND PROGESTERONE

8. Pain Management Associated With Endometriosis Peritoneal Endometriosis Ovarian Endometrioma Deep Nodular Endometriosis OCP Low Dose Estrogen NETA Dienogest 5mg/day 2mg/day <3cm >3cm Surgery OCP NETA + ABT If inefficacy or drug intolerance If inefficacy or drug intolerance > 33% Elgozon + ABT Surgery If inefficacy or drug intolerance To delay recurrence <2cm >3cm + ABT Surgery If inefficacy or drug intolerance 3 Months 3 Months Surgery OCP: Oral Contraceptive Pills NETA: Norethisterone acetate ABT: Add-Back Therapy Elgozon Elgozon Elgozon Elgozon

9. Mode of Action Elgozon Reduces levels of FSH and LH leading to decrease serum ESTRADIOL concentration. GnRH Gonadotropin Releasing Hormone GnRH Receptors Elgozon binds with GnRH Receptors FSH LH Ovary Elgozon Suppresses FSH and LH rapidly. Uterus Estradiol Elgozon 150mg QD Elgozon 200mg BID 42 pg/ml 12 pg/ml Median Estradiol Levels

10. Elgozon 150mg QD Elgozon 200mg BID 42 pg/ml 12 pg/ml Individually tailor treatment with 2 hormone-free dosing options that dial down estradiol to 2 different levels. Median Estradiol Levels (pg/ml)

11. Studies Suggested That Choosing Elgozon (ELAGOLIX) Symptoms of Endometriosis Benefit - Risk Bone loss/ vasomotor Symptoms 20 50 200 150 100 Estradiol (pg/ml) Partial Suppression Full Suppression Full Suppression + ABT Variable E2 Levels Understanding of Estradiol levels and Endometriosis Optimal estradiol suppression at 20-60 pg /ml balances efficacy, tolerance, and safety. Reference: https://www.mdpi.com/1422-0067/22/21/11342

12. WHY CHOOSE Elgozon (ELAGOLIX)? GnRH agonists (e.g., Leuprolide, Triptorelin, Goserelin) effectively treat endometriosis symptoms but have limitations, including: - Delayed therapeutic impact (7 to 14 days) - E2 suppression to less than 20 pg/mL - Inability to titrate E2 levels - Unpredictable reversibility Reference: https://www.mdpi.com/1422-0067/22/21/11342

13. WHY CHOOSE Elgozon (ELAGOLIX)? OCP administration reduced dysmenorrhea by approximately 50%, but showed no benefit for non-menstrual pelvic pain or dyspareunia. Reference: https://www.mdpi.com/1422-0067/22/21/11342

14. Elgozon(ELAGOLIX) - A Newer Treatment For Endometrial Pain Oral administration. Immediate suppression of FSH and LH within 24 hours after the initiation of treatment. Rapid reversibility of hormone secretion after stopping treatment.

15. Dysmenorrhea Reduction in Mean Dysmenorrhea Score -38% -47% -41% -14% -14% -19% PROVIDES PROVEN RELIEF ACROSS 3 MOST COMMON TYPES OF ENDOMETRIOSIS PAIN References: https://www.nejm.org/doi/10.1056/NEJMoa1700089

16. Non-Menstrual Pelvic Pain % of Women who reported reduced PELVIC PAIN between periods. 50% 55% 36% PROVIDES PROVEN RELIEF ACROSS 3 MOST COMMON TYPES OF ENDOMETRIOSIS PAIN References: https://ce.mayo.edu/sites/default/files/Orilissa%20hcp-patient-brochure.pdf

17. Elgozon was proven to reduce pain with sex in women who took the 200 mg dose, without increasing the use of painkillers. Dyspareunia PAIN WITH SEX PROVIDES PROVEN RELIEF ACROSS 3 MOST COMMON TYPES OF ENDOMETRIOSIS PAIN References: https://www.obgproject.com/2018/06/21/elaris-em-iii-elaris-em-iv-results-long-term-endometriosis-outcomes-following-administration-elagolix/

18. Elgozon (Elagolix) with add-back therapy is a potential treatment for women with heavy menstrual bleeding associated with uterine leiomyoma. Reference: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7253187/

19. ELGOZON (ELAGOLIX) WITH ADD-BACK THERAPY WAS EFFECTIVE IN REDUCING HEAVY MENSTRUAL BLEEDING IN WOMEN WITH UTERINE FIBROIDS % of Patients who has MBL volume of <80 ml & ≥50% reduction in MBL volume from baseline to the last 28 days before and including the last treatment period visit. Dose: 150mg two tablets BID 9% 84% 68.5% 10% 77% 77% Reference: https://www.nejm.org/doi/10.1056/NEJMoa1904351

20. ELGOZON (ELAGOLIX) WAS ASSOCIATED WITH REDUCTION IN FIBROID AND UTERINE VOLUMES Dose: 150mg two tablets BID Reference: https://www.sciencedirect.com/science/article/pii/S001502821730362X -36% +7% 36% reduction in the volume of largest fibroid by Elagolix . Change in Fibroid & Uterine Volume

21. Elgozon (ELAGOLIX) - Additional Benefits Reduces Fatigue Levels Improves Quality of Life Improves workplace & household productivity Reference: https://link.springer.com/article/10.1007/s40271-019-00394-7 , https://www.fertstert.org/article/S0015-0282(19)30146-3/fulltext# , https://journals.lww.com/greenjournal/fulltext/2020/09000/

22. PHARMACOKINETICS ABSORPTION DISTRIBUTION METABOLISM ELIMINATION Tmax = 1.0 h Effect of High-Fat Meal AUC = Decreases 24% Cmax = Decreases 36% % Drug Bound to Human Plasma Protein = 80% Half-life (t1/2) = 4 to 6 h Urine = < 3% feces = 90 % Hepatic Metabolism Major : CYP3A

23. Hot Flushes Amenorrhea Depression Night Sweats Insomnia ADVERSE EFFECTS

24. Pregnancy Osteoporosis Hypersensitivity CONTRAINDICATIONS

25. Should be discontinued if become pregnant. Should only be used if necessary. Safety and effectiveness has not been established. No dose adjustment is required renal impairment Recommend 150 mg in moderate & contraindicated in severe impairment. Equally safe in elderly patients Pregnancy Pediatrics Lactation Geriatrics Hepatic Impairment Renal Impairment USE IN SPECIAL POPULATION