TherapeuticsMD, Inc. (NYSE MKT: TXMD) - Pharmacokinetic study being
presented tomorrow evening in a poster session at The North American
Menopause Society 2013 Annual Meeting in Dallas suggests that the first
combination 17β-estradiol and progesterone capsule in clinical
development may have overcome the well-recognized difficulties of
achieving good bioavailability with oral administration of these
hormones in combination.
In a study of 66 healthy postmenopausal women, bioavailability of TX
12-001-HR, a capsule containing both 17β-estradiol and progesterone for
oral use being developed by TherapeuticsMD, Inc., was found to be
similar to that of the standard reference products for the human
hormones estradiol (Estrace®) and progesterone (Prometrium®),
when taken concurrently. Hormone therapy is widely used to alleviate the
symptoms of menopause and to reduce the health risks resulting from
hormone deficiencies associated with menopause.
“It has been notoriously difficult to combine these two body-identical
hormones and obtain consistently good bioavailability. And, when
compounding pharmacies create specialized blends of these hormones,
there is a great deal of variability in what is produced,” according to
James H. Pickar, M.D., Adjunct Associate Professor of Obstetrics and
Gynecology, Columbia University College of Physicians & Surgeons in New
York, who presented the study findings. In two FDA surveys of
compounding pharmacies, the amount of hormone found in the compounded
products was not the amount claimed in approximately 34% of compounded
products sampled and in 29% of hormone samples, versus the <2%
variability found for commercially manufactured products.1,2
In this study, bioequivalence criteria were met for all analytes, except
Cmax for total estrone. The extent of absorption of the
estradiol and progesterone in the Test capsule was similar to that for
Estrace and Prometrium, while the rate of estradiol absorption for the
Test capsule appeared to be slightly faster than for the Estrace
reference.
“The similarity in bioavailability of progesterone and estradiol in the
test product to that of the two reference products suggests that the
safety profile also should be similar,” Dr. Pickar said. Studies suggest
that products more closely resembling the human hormones progesterone
and estradiol may have a more favorable safety profile than synthetic
hormones.3,4 Dr. Pickar also noted that this investigational
therapy offers the additional advantage of avoiding use of the known
allergen, peanut oil, which is used in Prometrium and its generic
equivalents.
The need to ensure adequate bioavailability is critical for
progesterone, which protects the endometrium from estrogen stimulation.
“When progesterone levels are inadequate, women taking estrogen are put
at unnecessary risk for uterine cancer,” added Dr. Pickar.
About the Study
The study, which was sponsored by TherapeuticsMD, Inc., was designed to
determine the pharmacokinetics and bioavailability of the company’s
combination capsule of 17β-estradiol and progesterone (test drug:
TX12-001-HR). Participants included 66 healthy, postmenopausal women,
age 40-65 years. Each participant was randomly assigned to begin one of
three dosing sequences, each including three periods. During one period
participants received a single dose of the Test drug, and during two
periods they received single doses of both the estradiol and
progesterone Reference drugs, which were taken concurrently. Blood
samples were collected at multiple intervals, beginning one hour prior
to start of dosing and continuing to 48 hours after dosing.
Bioavailability was determined by measuring the rate and extent of
absorption of the drugs.
About Hormone Therapy
Menopausal hormone therapy (HT) is the administration of hormones to
treat menopausal symptoms resulting from a lack of naturally occurring
hormones. Current HT options include FDA-approved combination products,
FDA-approved estrogen-only and progestogen-only products, and non-FDA
approved compounded bioidentical products. A body-identical combination
product, which exactly matches the molecular structure of the human
hormones estradiol and progesterone, is being developed by
TherapeuticsMD and is currently in phase 3 clinical trials. HT is
projected to be the largest growth segment in the overall women’s health
market. The potential market for pharmacy-compounded, bioidentical HT
products is estimated to be approximately $1.5 billion per year.
About TX 12-001-HR
TX 12-001-HR is a body-identical investigational drug designed to treat
menopausal symptoms by replacing the 17ß-estradiol and progesterone
hormones the body has stopped producing as the result of menopause.
Enrollment is currently under way in the REPLENISH Trial, a Phase 3,
investigational research study made up of 1,550 patients to evaluate the
safety and efficacy of TX 12-001-HR in reducing the symptoms of
menopause. For more information, please visit: www.ReplenishTrial.com.
About TherapeuticsMD, Inc.
TherapeuticsMD, Inc. is a women’s healthcare company focused on
developing and commercializing products targeted exclusively for women.
We are currently developing advanced hormone therapy pharmaceutical
products designed to alleviate the symptoms of and reduce the health
risks resulting from menopause-related hormone deficiencies. We are also
evaluating various other potential indications for our hormone
technology, including oral contraception, preterm birth, vulvar and
vaginal atrophy, and premature ovarian failure. Additionally, our
business includes the manufacture and distribution of branded and
generic prescription prenatal vitamins, as well as over-the-counter
vitamins and cosmetics, under our vitaMedMD® and BocaGreenMD™
brands. More information is available at the following websites: www.therapeuticsmd.com,
www.vitamedmd.com,
www.vitamedmdrx.com,
and www.bocagreenmd.com.
vitaMedMD® and TherapeuticsMD® are registered
trademarks of TherapeuticsMD, Inc. BocaGreenMD™ is a trademark of
TherapeuticsMD, Inc.
Except for the historical information contained herein, the matters
set forth in this press release, including statements regarding the
continuation and ultimate results of clinical development of the
Company’s proposed combination17β-estradiol and progesterone drug, the
use of hormone therapy to alleviate the symptoms of menopause and to
reduce the health risks resulting from hormone deficiencies associated
with menopause, the critical need to ensure adequate
bioavailability for progesterone, the Company’s belief in the attributes
and the expected benefits of TX 12-001HR, what the TX 12-001HR clinical
trial is designed to measure, and the potential size of the HT market
are forward-looking statements within the meaning of the “safe harbor”
provisions of the Private Securities Litigation Reform Act of 1995.
These forward-looking statements are subject to risks and uncertainties
that may cause actual results to differ materially, including but not
limited to: timely and successful completion of clinical studies and the
results thereof; risks and uncertainties associated with the Company’s
business and finances in general; and other risks detailed in the
Company’s filings with the U.S. Securities and Exchange Commission
including its annual report on Form 10-K, reports on Form 10-Q and Form
8-K, and other such filings. These forward-looking statements are based
on current information that may change. Investors are cautioned not to
place undue reliance on these forward-looking statements, which speak
only as of the date of this press release. All forward-looking
statements are qualified in their entirety by this cautionary statement,
and the Company undertakes no obligation to revise or update any
forward-looking statement to reflect events or circumstances after the
issuance of this press release.
References
1. Food and Drug Administration. Report: Limited FDA survey of
compounded drug products. Available at: http://www.fda.gov/Drugs/GuidanceComplianceRegulatoryInformation/PharmacyCompounding/ucm155725.htm
Accessed on September 19, 2013
2. Food and Drug Administration. Report: 2006 limited FDA survey of
compounded drug products. Available at: http://www.fda.gov/Drugs/GuidanceComplianceRegulatoryInformation/PharmacyCompounding/ucm204237.htm
Accessed on July 19, 2013
3. Fournier A, Berrino F, Clevel-Chapelon F. Unequal risks for breast
cancer associated with different hormone replacement therapies: results
from E3N cohort study. Breast Cancer Res Treat 2008;107:103-111.
4. The Writing Group for the PEPI Trial. Effects of estrogen or
estrogen/progestin regimens on heart disease risk factors in
postmenopausal women. The postmenopausal estrogen/progestin
interventions (PEPI) trial. JAMA 1995;273(3):199-208.
Copyright Business Wire 2013