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Ulipristal

Generic Name
Ulipristal
Brand Names
Ella, Ellaone, Esmya, ellaOne
Drug Type
Small Molecule
Chemical Formula
C28H35NO3
CAS Number
159811-51-5
Unique Ingredient Identifier
6J5J15Q2X8

Overview

Ulipristal is a selective progesterone receptor modulator used for the purposes of emergency contraception (Ella) and for the treatment of uterine fibroids (Fibristal). It is a derivative of 19-norprogesterone and has both antagonistic and partial agonist activity at the progesterone receptor. It also binds to glucocorticoid receptor, however compared to mifepristone (a progesterone receptor antagonist), ulipristal is more tolerable and has lower glucocorticoid activity and better binding affinity. Ulipristal is currently recommended as first line therapy for emergency contraception, due to improved efficacy and similar side effect profile as compared to the traditional use of levonorgestrel or the Yuzpe regimen. The exact mechanism of action for ulipristal is still currently debated, though there is evidence that it functions by inhibiting ovulation. A recent systematic review proclaimed that the majority of available evidence demonstrates an inhibitory effect on ovulation rather than a post-fertilization effect on the endometrium, which has been heavily debated due to ethical concerns related to abortion (Rosato et al, 2016). Nevertheless, current and ongoing research into the agent's mechanism of action as an emergency contraceptive continue to provide potentially plausible evidence that ulipristal may, in fact, elicit activity on the endometrium that prevents embryo implantation .

Background

Ulipristal is a selective progesterone receptor modulator used for the purposes of emergency contraception (Ella) and for the treatment of uterine fibroids (Fibristal). It is a derivative of 19-norprogesterone and has both antagonistic and partial agonist activity at the progesterone receptor. It also binds to glucocorticoid receptor, however compared to mifepristone (a progesterone receptor antagonist), ulipristal is more tolerable and has lower glucocorticoid activity and better binding affinity. Ulipristal is currently recommended as first line therapy for emergency contraception, due to improved efficacy and similar side effect profile as compared to the traditional use of levonorgestrel or the Yuzpe regimen. The exact mechanism of action for ulipristal is still currently debated, though there is evidence that it functions by inhibiting ovulation. A recent systematic review proclaimed that the majority of available evidence demonstrates an inhibitory effect on ovulation rather than a post-fertilization effect on the endometrium, which has been heavily debated due to ethical concerns related to abortion (Rosato et al, 2016). Nevertheless, current and ongoing research into the agent's mechanism of action as an emergency contraceptive continue to provide potentially plausible evidence that ulipristal may, in fact, elicit activity on the endometrium that prevents embryo implantation .

Indication

As the product Ella (available in Canada and the US), ulipristal is indicated for use as emergency contraception after unprotected intercourse or possible contraceptive failure when administered within 120 hours (5 days) after unprotected intercourse or a known or suspected contraceptive failure. As the product Fibristal (available in Canada), ulipristal is indicated for treatment of the signs and symptoms of uterine fibroids in adult women.

Associated Conditions

  • Moderate Uterine Fibroids
  • Severe Uterine Fibroids

FDA Drug Approvals

Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
HRA PHARMA AMERICA, INC.
73302-456
ORAL
30 mg in 1 1
11/1/2023
RPK Pharmaceuticals, Inc.
53002-2630
ORAL
30 mg in 1 1
5/11/2020
RedPharm Drug, Inc
67296-1466
ORAL
30 mg in 1 1
2/15/2023
RPK Pharmaceuticals, Inc.
53002-1630
ORAL
30 mg in 1 1
5/10/2018
A-S Medication Solutions
50090-2835
ORAL
30 mg in 1 1
5/10/2018
A-S Medication Solutions
50090-5422
ORAL
30 mg in 1 1
5/11/2020

HSA Drug Approvals

Approved Product
Manufacturer
Approval Number
Dosage Form
Strength
Approval Date
ELLA TABLET 30MG
SIN13979P
TABLET
30.00 mg
6/21/2011

NMPA Drug Approvals

Approved Product
Company
Approval Number
Drug Type
Dosage Form
Approval Date
No NMPA approvals found for this drug.

PPB Drug Approvals

Approved Product
Registration No.
Company
Licence No.
Strength
Registration Date
No PPB approvals found for this drug.

TGA Drug Approvals

Approved Product
ARTG ID
Sponsor
Registration Type
Status
Registration Date
EllaOne ulipristal acetate 30 mg tablet blister pack
219535
Medicine
A
3/6/2015
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