Estradiol

Articles · Lactation Safety Information · New Medicines ·
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Articles

Lactation Safety Information

As a contraceptive when combined with a progestogen

As a contraceptive when combined with a progestogen
Progestogen-only contraceptive
Avoid in infants aged up to 6 weeks. Use with caution in infants aged over 6 weeks - a progestogen-only contraceptive preferred during lactation at any stage – see summary
24th September 2020

New Medicines

Lenzetto · Hormone replacement therapy for estrogen deficiency symptoms in postmenopausal women

Information

Lenzetto
New formulation
Gedeon Richter
Not Known

Development and Regulatory status

Launched
Launched
None
April 2020
Apr 20 · Launched in UK. Price: 1.53mg per metered dose transdermal spray, 8.1ml (56 actuations)=£6.90. Lenzetto is the first transdermal spray to be licensed in the UK for management of oestrogen deficiency symptoms in postmenopausal women [5].
Mar 20 · Is also licensed and available in other European countries, approved using a non-centralised procedure (MRP or DCP) [3,4].
Aug 15 · Approved in UK for use as hormone replacement therapy (HRT) for estrogen deficiency symptoms in postmenopausal women (in women at least 6 months since last menses or surgical menopause, with or without a uterus) [2].

Category

Synthetic 17β-estradiol, chemically and biologically identical to endogenous human estradiol. In a transdermal spray which is applied to the forearm once daily.
Many women do not seek medical advice for menopausal symptoms. Variations in consultation patterns for menopause depend on many factors, including cultural and educational differences as well as psychosocial difficulties. Around 80% of women going through their menopause experience symptoms and around a quarter have severe symptoms, but only a small proportion of menopausal women take hormone replacement therapy (HRT) [1].
Hormone replacement therapy for estrogen deficiency symptoms in postmenopausal women
Transdermal

Evidence based evaluations

SPC

Imvexxy · Vulvovaginal or vaginal atrophy-associated moderate-to-severe vaginal pain during sexual intercourse (dyspareunia) in postmenopausal women - vaginal formulation [2].

Information

Imvexxy
New formulation VagiCap™ softgel capsule
Theramex
TherapeuticsMD

Development and Regulatory status

None
None
Launched
Jun 19 · TherapeuticsMD enters into a exclusive license and supply agreement with Theramex to commercialise Imvexxy outside of the US, excluding Canada and Israel, for which TherapeuticsMD has licensed Imvexxy to Knight Therapeutics [5].
Sep 18 · Launched in the US [5].
May 18 · FDA approval of Imvexxy (estradiol vaginal inserts 4mcg and 10mcg) for the treatment of moderate-to-severe dyspareunia, is based on the results from the PIII REJOICE trial [5].
May 18 · Approved in US [4].
Dec 17 · Therapeutics MD resubmitted the New Drug Application (NDA) to the US FDA for Yuvvexy (applicator-free estradiol vaginal softgel capsule) for moderate-to-severe dyspareunia due to menopause.[4]
Nov 17 · The FDA have now agreed to waive the preapproval safety study, as long as the company agrees to postapproval observational study to monitor safety. TherapeuticsMD plan to resubmit for filing with the FDA in 2017.[3]
Sep 17 · TherapeuticsMD submitted additional endometrial long-term safety information to support its NDA for estradiol vaginal.[2,3]
May 17 · TherapeuticsMD receives complete response letter from US FDA in which 12-month safety data (rather than the 12 weeks worth of data submitted) were requested. The main point of concern for the FDA was endometrial safety. [2,3]
Feb 17 · TherapeuticsMD has patents pending for Estradiol vaginal in Europe.[2]
Sep 16 · Accepted for review by US FDA. [2]
Jul 16 · Filed for approval to US FDA. [2,3]

Category

Oestrogen receptor antagonist formulated as low dose estradiol VagiCap™ softgel capsule
80% of women experience menopausal symptoms and 45% find it distressing. Symptoms include hot flushes, night sweats, increase in weight and vaginal atrophy. Vaginal atrophy occurs because of reduced endogenous oestrogen production, leading to the vaginal walls to become thin and dry. This may lead to itchiness, discomfort, pain during intercourse, vaginal discharge, and urinary problems. About 30% of women experience vaginal symptoms in the early postmenopausal period and 47% post menopause [1].
Vulvovaginal or vaginal atrophy-associated moderate-to-severe vaginal pain during sexual intercourse (dyspareunia) in postmenopausal women - vaginal formulation [2].
Vaginal

Trial or other data

Oct 15 · PIII REJOICE Trial (NCT02253173) completed. The 12-week, randomised, double-blind, placebo-controlled trial evaluated safety and efficacy of estradiol vaginal (25µg, 10µg and 4µg), in 764 pts with symptoms of vulval vaginal atrophy (VVA) (including dyspareunia), due to menopause. All doses demonstrated significant change from baseline in the % of vaginal superficial cells, % of vaginal parabasal cells, vaginal pH and self-reported severity of dyspareunia. Vaginal dryness was reduced by all doses at weeks 2, 6, 8 and 12. For all the three doses, statistical improvement vs. placebo was seen at week 2 through week 12. After 12 weeks, FSFI scores increased signficantly at the 10mcg and 25mcg doses vs. placebo. The results demonstrated negligible to very low systemic absorption of estradiol vaginal. Estradiol vaginal was well tolerated. Adverse events were headache, vaginal discharge, nasopharyngitis and vulvovaginal pruritus. No drug-related serious adverse events were reported [2].