Consumer medicine information

Orgalutran

Ganirelix

BRAND INFORMATION

Brand name

Orgalutran

Active ingredient

Ganirelix

Schedule

S4

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using Orgalutran.

What is in this leaflet

This leaflet answers some common questions about Orgalutran.

It does not contain all the available information. It does not take the place of talking to your doctor or pharmacist.

All medicines have risks and benefits. Your doctor has weighed the risks of you taking Orgalutran against the benefits they expect it will have for you.

If you have any concerns about using this medicine, ask your doctor or pharmacist.

Keep this leaflet with the medicine. You may need to read it again.

What Orgalutran is used for

Orgalutran is used together with other medications to regulate hormone response in women undergoing Assisted Reproductive Technology such as in vitro fertilisation (IVF).

Orgalutran works by preventing women from ovulating (releasing an egg from the ovary) too soon during stimulation of their ovaries to produce a mature egg.

Ask your doctor if you have any questions about why this medicine has been prescribed for you.

No effects on ability to drive and use machines have been observed.

Orgalutran is not addictive.

This medicine is available only with a doctor's prescription.

Before you use Orgalutran

When you must not use it

Do not use Orgalutran if:

  • you are allergic (hypersensitive) to ganirelix or to any other components of Orgalutran, including the ingredients listed at the end of this leaflet and/or dry natural rubber/latex
  • you are allergic to any other similar medicines
  • you are pregnant
  • you are breastfeeding
  • you have moderate to severe kidney or liver disease
  • the solution is not clear and colourless
  • the expiry date on the pack has passed
  • the package shows any signs of tampering

If you are not sure whether you should start using Orgalutran, talk to your doctor.

Before you start to use it

Tell your doctor if :

  • you have allergies to any other medicines, substances such as foods, preservatives or dyes
  • you are currently experiencing allergic symptoms
  • you have any other medical conditions

Cases of allergic reactions, both generalised and local, including hives (urticaria), swelling of the face, lips, tongue and/or throat that may cause difficulty in breathing or swallowing (angioedema and/or anaphylaxis) have been reported, as early as with the first dose. (See also Side Effects). If you have an allergic reaction, stop taking Orgalutran and seek immediate medical assistance.

The needle shield of Orgalutran contains dry natural rubber/ latex which comes into contact with this product and may cause allergic reactions.

Taking other medicines

Tell your doctor if you are taking any other medicines, including any that you get without a prescription from your pharmacy, supermarket or health food shop.

How to use Orgalutran

Treatment with Orgalutran should be started under the supervision of a fertility specialist.

Orgalutran is given as a subcutaneous (under the skin) injection in the thigh or stomach.

The injection site should be changed every day to lessen possible injection site reactions.

If your doctor or nurse decides you can give the injections yourself, they will teach you the injection technique.

Do not attempt self-injection until you are sure of how to do it.

Follow all instructions given to you by your doctor or nurse carefully.

How much to inject

The usual dose is the contents of one pre-filled syringe of Orgalutran once a day on specific days of the menstrual cycle. Your doctor will tell you when to inject Orgalutran.

You may notice air bubbles in the pre-filled syringe. This is expected, and removal of the air bubbles is not needed.

How to use Orgalutran

Follow these steps:

  1. Prepare the injection site
Wash your hands thoroughly with soap and water. Swab the injection site with a disinfectant to remove any surface bacteria. Clean about 5 cm around the point where the needle will go in. Let the disinfectant dry for at least one minute before proceeding.
  1. Open the outer pack and plastic container inside
While waiting for the disinfectant to dry, open the Orgalutran pack and remove the plastic container. Carefully open the plastic container and remove the Orgalutran syringe. You will see the needle is already attached, covered by a grey needle shield.
  1. Prepare the syringe for injection
Remove needle shield and discard it in a sharps-disposable bin. You are now ready to inject Orgalutran.
  1. Inserting the needle and injecting
Orgalutran is injected in either the thigh or the abdomen, usually near the navel.
Pinch up a large bit of skin between your finger and thumb. Insert the needle at the base of the pinched-up skin at an angle of 45 degrees to 90 degrees to the skin surface. Gently draw back on the plunger to see if the needle is inserted correctly.
If any blood appears in the syringe, the needle is not inserted correctly so do not inject Orgalutran. Remove the needle, cover the injection site with a sterile swab and dispose of the syringe in a sharps-disposable container. Start again with a new syringe.
If the needle has been inserted correctly, depress the plunger slowly and steadily until all the solution has been injected.
Vary the injection site each time to minimise local irritation.
  1. Removing the needle
Pull the needle out of the skin quickly and apply pressure to the site with a swab containing disinfectant. Dispose of the syringe (with the attached needle) in a Sharps Container.

Use the syringe only once and then dispose of it in the Sharps Container.

How long to use Orgalutran

Your doctor will tell you when to inject Orgalutran and when to stop injecting it.

If you forget to use Orgalutran

If you forget an injection, contact your doctor or IVF clinic immediately for advice.

Do not inject a double-dose to make up for the forgotten dose.

If you inject too much

Immediately contact your doctor or IVF clinic, or for Australia, the Poisons Information Centre (telephone 131 126), or for New Zealand, National Poisons Centre (telephone 0800 POISON or 0800 764 766) for advice if you think you have given yourself too much Orgalutran.

While you are Using Orgalutran

Things you must do

Contact your doctor immediately if you have severe pelvic pain, nausea and vomiting and weight gain.

These are early warning signs of Ovarian Hyperstimulation Syndrome (OHSS).

Other symptoms of OHSS can include:

  • indigestion
  • diarrhoea
  • shortness of breath
  • reduced amounts of urine
  • painful breast

OHSS is a possible complication of hormonal stimulation of the ovaries.

Keep all of your doctor's appointments so that your progress can be checked. Your doctor will want to follow the developing eggs inside the ovaries by doing an ultrasound examination and measuring hormones in your blood.

Make sure that all doctors, dentists and pharmacists who are treating you know you are using Orgalutran.

Tell the hospital doctor that you are using Orgalutran if you need to have an operation, or go to hospital in an emergency.

If you are about to be started on any new medicine, tell your doctor or pharmacist that you are using Orgalutran.

Things you must not do

If you are self injecting:

  • do not stop using Orgalutran without telling your doctor
  • do not change the dose unless your doctor tells you to

Changing your dose without telling your doctor can increase your risk of unwanted side effects or can prevent the drug from working properly.

Do not give this medicine to anyone else, even if they have the same condition as you.

Do not use this medicine to treat any other complaints.

Things to be careful of

Compared to natural conception, the frequency of multiple pregnancies and births is increased in patients undergoing assisted reproductive techniques. Discuss the risk of multiple pregnancies and births with your doctor.

Side Effects

Tell your doctor or pharmacist as soon as possible if you do not feel well while taking Orgalutran.

All medicines can have side effects. Sometimes they are serious, most of the time they are not. You may need medical treatment if you get some of the side effects.

Tell your doctor if you notice any of the following and they worry you:

  • redness, pain or swelling at injection site. Usually these symptoms disappear within a few hours after injection.
  • headache
  • nausea
  • tiredness

Tell your doctor immediately if you notice any of the following:

  • shortness of breath, wheezing, difficulty breathing or a tight feeling in your chest
  • swelling of the face, lips, tongue and/or throat that may cause difficulty in breathing or swallowing (angioedema and/or anaphylaxis), or other parts of the body
  • rash, itching, hives (urticaria) or flushed, red skin

This list includes very serious side effects that have been observed, as early as with the first dose. You may need urgent medical attention or hospitalisation. These side effects are rare.

Other side effects are known to occur with Assisted Reproductive Technology (ART) procedures. These may include:

  • Ovarian Hyperstimulation Syndrome. Since overstimulation can occur rapidly you must contact your doctor if you experience any of the following: pain in the abdomen or pelvis, indigestion, nausea, vomiting, weight gain, shortness of breath, reduced amounts of urine, diarrhoea and painful breasts.
  • vaginal bleeding
  • miscarriage
  • ectopic pregnancy

The incidence of ectopic pregnancies (embryo implanted outside the womb) may be increased in women undergoing ART. Your doctor will perform an ultrasound scan early during pregnancy to confirm that a pregnancy is intrauterine (in the womb).

These side effects are probably unrelated to treatment with Orgalutran.

The incidence of congenital malformations (a physical defect present in a baby at birth) after ART may be slightly higher than after spontaneous conceptions. The slightly higher incidence is thought to be related amongst other factors to characteristics of the patients undergoing fertility treatment (e.g. age of the female, sperm characteristics) and to the higher incidence of multiple gestations after ART. The incidence of congenital malformations after ART using Orgalutran is not different from that after using other GnRH analogues in the course of ART.

Tell your doctor if you notice anything that is making you feel unwell. Other side effects not listed above may occur in some people.

After Using Orgalutran

Storage

Keep Orgalutran in a safe place away from the sight and reach of children. A locked cupboard at least one-and-a-half-metres above the ground is a good place to store medicines.

Keep Orgalutran below 30°C. Do not put it in the freezer as the syringe may break.

Keep the syringe in the outer carton to protect it from light.

Disposal

Dispose of your Orgalutran syringe and needle safely into a yellow plastic Sharps Container.

If your doctor tells you to stop using Orgalutran or the expiry date has passed, ask your pharmacist or IVF clinic what to do with any Orgalutran that is left over.

Product Description

What Orgalutran looks like

Orgalutran is a clear colourless solution. It comes in a pre-filled syringe with fixed needle closed by a needle shield of dry natural rubber/ latex which comes into contact with this product.

Ingredients

  • each syringe contains 250 microgram of ganirelix
  • inactive ingredients are acetic acid, mannitol and water for injections

Orgalutran is available in packs of 1 or 5 pre-filled syringes.

Identification

Orgalutran can be identified by the Australian Register Number on the carton: AUST R 74931

Distributed by

Organon Pharma Pty Ltd
Building A, 26 Talavera Rd
Macquarie Park NSW 2113
Australia

Date leaflet revised:
November 2022

RCN000015270

Published by MIMS December 2022

BRAND INFORMATION

Brand name

Orgalutran

Active ingredient

Ganirelix

Schedule

S4

 

1 Name of Medicine

Ganirelix acetate.

2 Qualitative and Quantitative Composition

Orgalutran 250 microgram ganirelix (as acetate)/0.5 mL solution for injection.

Orgalutran contains the synthetic decapeptide ganirelix (INN) as its acetate salt, with high antagonistic activity to the naturally occurring gonadotropin releasing hormone (GnRH).
Each prefilled syringe contains 250 microgram ganirelix (as acetate) in 0.5 mL.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Solution for injection.
Orgalutran (ganirelix acetate) is presented as a sterile, ready for use, clear and colourless aqueous solution intended for subcutaneous administration.

4 Clinical Particulars

4.1 Therapeutic Indications

For the prevention of premature luteinisation and ovulation in patients undergoing controlled ovarian stimulation, followed by oocyte pick up and assisted reproductive techniques.

4.2 Dose and Method of Administration

Orgalutran should only be prescribed by a specialist experienced in the treatment of fertility.

Dosage.

Orgalutran is used to prevent premature LH surges in patients undergoing COH. Controlled ovarian hyperstimulation with FSH may start at day 2 or 3 of menses. Orgalutran (0.25 mg) should be injected subcutaneously once daily, starting from day 5 or day 6 of FSH administration depending on the level of ovarian response. Orgalutran should not be mixed with FSH but both preparations should be administered approximately at the same time. Daily treatment with Orgalutran should be continued up to the day that sufficient follicles of adequate size are present. Final maturation of follicles can be induced by administering hCG. Because of the half life of ganirelix, the time between two Orgalutran injections and between the last Orgalutran injection and the hCG injection should not exceed 30 hrs, as otherwise a premature LH surge may occur.

Method of administration.

Inspect the solution before use. It must only be used if it is clear and without particulate matter.
Orgalutran should be administered subcutaneously. The injection site should be varied to prevent lipoatrophy. The patient or her partner may perform the injections of Orgalutran themselves, provided that they are adequately instructed and have access to expert advice. Air bubble(s) may be seen in the pre-filled syringe. This is expected, and removal of the air bubble(s) is not needed.

4.3 Contraindications

Hypersensitivity to the active substance or to any of the components including dry natural rubber/latex (see Section 6.1 List of Excipients; Section 6.5 Nature and Contents of Container).
Hypersensitivity to GnRH or any other GnRH analogue.
Pregnancy or lactation.
Moderate to severe renal impairment and hepatic impairment.

4.4 Special Warnings and Precautions for Use

Special care should be taken in women with signs and symptoms of active allergic conditions. Cases of hypersensitivity reactions (both generalised and local), have been reported with Orgalutran, as early as with the first dose, during post-marketing surveillance. These events have included anaphylaxis (including anaphylactic shock), angioedema, and urticaria (see Section 4.8 Adverse Effects (Undesirable Effects)). If a hypersensitivity reaction is suspected, Orgalutran should be discontinued and appropriate treatment administered. Use of Orgalutran in patients with active allergic symptoms has not been investigated. Administration of Orgalutran is not advised to patients with currently severe allergic symptoms. Patients should be advised to contact the attending physician before administering the next injection in case a general or an extensive local allergic reaction occurs.
The needle shield of Orgalutran contains dry natural rubber/latex which comes into contact with this product and may cause allergic reactions (see Section 4.3 Contraindications; Section 6.5 Nature and Contents of Container).
Ovarian hyperstimulation syndrome (OHSS) may occur during or following ovarian stimulation. OHSS must be considered an intrinsic risk of gonadotrophin stimulation. OHSS should be treated symptomatically, e.g. with rest, intravenous infusion of electrolyte solutions or colloids and heparin.
Since infertile women undergoing assisted reproduction, and particularly IVF, often have tubal abnormalities, the incidence of ectopic pregnancies might be increased. Early ultrasound confirmation that a pregnancy is intrauterine is therefore important.
The safety and efficacy of Orgalutran have not been established in women weighing less than 50 kg or more than 90 kg.

Congenital abnormalities.

The incidence of congenital malformations after Assisted Reproductive Technologies (ART) may be slightly higher than after spontaneous conceptions. This slightly higher incidence is thought to be related amongst other factors, to differences in parental characteristics (e.g. maternal age, sperm characteristics) and by the higher incidence of multiple gestations after ART. In clinical trials investigating more than 1000 newborns, it has been demonstrated that the incidence of congenital malformation in children born after Controlled Ovarian Hyperstimulation (COH) treatment using Orgalutran is comparable with that reported after COH treatment using a GnRH agonist.

Use in hepatic impairment.

See Section 4.3 Contraindications.

Use in renal impairment.

See Section 4.3 Contraindications.

Use in the elderly.

No data available.

Paediatric use.

There is no relevant use of Orgalutran in the paediatric population.

Effects on laboratory tests.

No data available.

4.5 Interactions with Other Medicines and Other Forms of Interactions

In clinical studies, interactions of Orgalutran with other medicines have not been investigated. Therefore, interactions with commonly used medicinal products can not be excluded.
In the absence of incompatibility studies, this medicinal product must not be mixed with other medicinal products.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

Ganirelix treatment of female rats resulted in reversible impairment of mating and fertility at a subcutaneous dose of 2.5 microgram/kg/day, and reversible cessation of mating was seen in males treated with a subcutaneous dose of 0.1 mg/kg/day.
(Category D)
Orgalutran is not intended to be used during pregnancy (see Section 4.3 Contraindications). No clinical data on exposed pregnancies are available.
Studies in animals have indicated that ganirelix increased the incidence of total fetal resorptions when administered to pregnant rats and rabbits during the period of organogenesis, at respective doses of 10 microgram/kg/day and 30 microgram/kg/day (approximately 0.4 and 3 times the human dose, based on body surface area). The effects on fetal resorption are logical consequences of the alteration in hormonal levels brought about by the antigonadotrophic properties of Orgalutran and could result in fetal loss in humans. There was no increase in fetal abnormalities. No treatment related changes in fertility, physical or behavioural characteristics were observed in the offspring of female rats treated with ganirelix during pregnancy and lactation.
 Orgalutran should not be used by lactating women (see Section 4.3 Contraindications). It is not known whether ganirelix is excreted into animal or human breast milk. Subcutaneous ganirelix doses of 2.5 microgram/kg/day given to lactating rats did not result in impairment of postnatal development of the offspring.

4.7 Effects on Ability to Drive and Use Machines

The effects of this medicine on a person's ability to drive and use machines were not assessed as part of its registration.

4.8 Adverse Effects (Undesirable Effects)

General disorders and administrative site conditions.

Orgalutran may cause a skin reaction (in 10% - 15% of the patients moderate or severe redness with or without swelling was reported) at the site of injection, which normally disappears within 4 hours after administration. Malaise was reported in 0.3% of patients.

Immune system disorders.

Very rarely, post-marketing cases of hypersensitivity reactions (including rash, facial swelling, dyspnea, anaphylaxis (including anaphylactic shock), angioedema, and urticaria) have been reported, as early as with the first dose, among patients administered Orgalutran.

Nervous system disorders.

Headache (0.4%).

Gastrointestinal disorders.

Nausea (0.5%).
Other reported adverse events are rather related to the controlled ovarian hyperstimulation treatment for assisted reproduction technique (ART) than to Orgalutran (e.g. pelvic pain, abdominal distension, ovarian hyperstimulation syndrome (OHSS), ectopic pregnancy and spontaneous abortion).

Reporting suspected adverse effects.

Reporting suspected adverse reactions after registration of the medicinal product is important. It allows continued monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions at http://www.tga.gov.au/reporting-problems.

4.9 Overdose

Overdosage in humans may result in a prolonged duration of action. In case of overdose, Orgalutran treatment should be (temporarily) discontinued.
No data on acute toxicity of Orgalutran in humans are available. Clinical studies with subcutaneous administration of Orgalutran at single doses up to 12 mg did not show systemic side-effects. Clinical signs of systemic toxicity including collapse, laboured respiration and inactivity in rats or facial flushing in monkeys were observed after intravenous administration of ganirelix at 2.0 and 3.0 mg/kg, respectively. Blood pressure was also reduced by about 50% in rats treated with an intravenous ganirelix dose of 0.9 mg/kg.
For information on the management of overdose, contact the Poisons Information Centre on 131126 (Australia).

5 Pharmacological Properties

5.1 Pharmacodynamic Properties

Pharmacotherapeutic group: anti-gonadotrophin releasing hormone; ATC code: H01CC01.

Mechanism of action.

Orgalutran is a GnRH antagonist, which modulates the hypothalamic-pituitary-gonadal axis by competitively binding to the GnRH receptors in the pituitary gland. As a result a rapid, reversible suppression of endogenous gonadotropins occurs, without initial stimulation as induced by GnRH agonists. The inhibitory effect of Orgalutran on the release of LH is more pronounced than on FSH. When LH has started to rise prior to the first administration of Orgalutran, a premature LH surge can still be prevented.
Important features of the GnRH-antagonist regimen:
within a few hours suppression of gonadotropin release due to GnRH receptor blockade;
Orgalutran treatment is restricted to those days when a premature LH surge may occur. Therefore, the overall duration of treatment is only several days;
less suppression of endogenous FSH and therefore less FSH required;
recovery of pituitary functioning within two days following discontinuation of the treatment;
the competitive mode of action of Orgalutran may allow the administration of a GnRH agonist instead of hCG to trigger ovulation, which is especially relevant for patients at risk of developing OHSS;
generally, estradiol levels are lower (though remaining above natural cycle levels) compared to the relatively high levels in the agonist regimen.

Clinical trials.

The efficacy of Orgalutran (ganirelix acetate) was established in three clinical studies. In these studies, the administration of exogenous recombinant FSH [Puregon (follitropin beta for injection)] was initiated on the morning of Day 2 or 3 of a natural menstrual cycle. Orgalutran was administered on the morning of Day 7 or 8 (Day 6 of recombinant FSH administration). The dose of recombinant FSH administered was adjusted according to individual responses starting on the day of initiation of Orgalutran. Both recombinant FSH and Orgalutran were continued daily until at least three follicles were 17 mm or greater in diameter at which time hCG [Pregnyl (chorionic gonadotropin for injection)] was administered. Following hCG administration, Orgalutran and recombinant FSH administration were discontinued. Oocyte retrieval, followed by in vitro fertilisation (IVF) or intracytoplasmic sperm injection (ICSI), was subsequently performed.
In a multicenter, double blind, randomised, dose finding study (protocol 38602), Orgalutran doses ranging from 62.5 microgram to 2,000 microgram and recombinant FSH were administered to 332 patients undergoing COH for IVF. The results of the selected dose (250 microgram) are summarized in Table 1.
Two multicentre, open-label, randomised studies (protocol 38607 and 103-001) were conducted in which follicular phase treatment with Orgalutran 250 microgram was studied using a GnRH agonist as a reference treatment. A total of 661 subjects were treated with Orgalutran by subcutaneous injection once daily starting on Day 6 of recombinant FSH treatment. Recombinant FSH was maintained at 150 IU or 225 IU in the 38607 and 103-001 study, respectively for the first 5 days of ovarian stimulation and was then adjusted by the investigator on the sixth day of gonadotropin use according to individual responses. The results for the Orgalutran arm are summarized in Table 1.
In subjects administered Orgalutran 250 microgram, a premature LH surge prior to hCG administration, (LH rise ≥ 10 mIU/mL with a significant rise in serum progesterone > 2 nanogram/mL, or a significant decline in serum estradiol) occurred in less than 1% of subjects.
In case of high ovarian response, as assessed by the number and size of growing follicles and/or the amount of circulating estradiol, either as a result of a high FSH exposure in the early follicular phase or as a result of high ovarian responsiveness, premature LH rises may occur earlier than day 6 of stimulation. Initiation of Orgalutran treatment on day 5 can effectively prevent these premature LH rises without compromising the clinical outcome.

5.2 Pharmacokinetic Properties

Absorption.

After a single subcutaneous administration of 250 microgram, serum levels of ganirelix rise rapidly and reach peak levels (Cmax) of approximately 15 nanogram/mL within 1 to 2 hrs (tmax). The bioavailability of Orgalutran following subcutaneous administration is approximately 91%.
Pharmacokinetic parameters after multiple subcutaneous dosing of Orgalutran (once daily injection) were similar to those after a single subcutaneous dose. After repeated dosing at 0.25 mg/day, steady-state levels of approximately 0.6 nanogram/mL were reached within 2 to 3 days.

Distribution.

The mean (SD) volume of distribution of Orgalutran in healthy females following intravenous administration of a single 250 microgram dose is approximately 44 (± 11) liters. In vitro protein binding to human plasma is approximately 82%.

Metabolism.

The major circulating component in plasma is ganirelix. Ganirelix is also the main compound found in urine, and faeces only contained metabolites.

Excretion.

After a single subcutaneous administration of 250 microgram, the elimination half-life (t1/2) is approximately 13 hrs and clearance is approximately 2.4 L/h.
In a radiolabelled study (n = 3), Orgalutran was excreted via faeces (approximately 75%) and urine (approximately 22%).

5.3 Preclinical Safety Data

Genotoxicity.

Ganirelix showed no evidence of genotoxicity in assays for gene mutation in bacterial or mammalian cells. Ganirelix was not clastogenic in tests for chromosomal damage in Chinese hamster ovary cells in vitro and for micronucleus formation in mice in vivo.

Carcinogenicity.

Long-term carcinogenicity studies with ganirelix have not been carried out.

6 Pharmaceutical Particulars

6.1 List of Excipients

The Orgalutran solution for injection also contains acetic acid, mannitol and water for injection. The pH may have been adjusted with sodium hydroxide and/or acetic acid.

6.2 Incompatibilities

See Section 4.5 Interactions with Other Medicines and Other Forms of Interactions.

6.3 Shelf Life

36 months.

6.4 Special Precautions for Storage

Store at room temperature below 30°C in the original package. Do not freeze as the syringe may break. Protect from light.

6.5 Nature and Contents of Container

Orgalutran is supplied in disposable prefilled syringes (siliconised Type I glass), containing 250 microgram ganirelix/0.5 mL. Each prefilled syringe is affixed with a needle closed by a needle shield of dry natural rubber/latex which comes into contact with this product (see Section 4.3 Contraindications; Section 4.4 Special Warnings and Precautions for Use).
Boxes of Orgalutran contain 1 or 5 prefilled syringes.
Australian Registration No.: AUSTR 74931.

6.6 Special Precautions for Disposal

This product is for single use only. Discard any remaining contents.
Any unused product or waste material should be disposed of in accordance with local requirements.

6.7 Physicochemical Properties

The amino acids at positions 1, 2, 3, 6, 8 and 10 of the natural GnRH decapeptide have been substituted resulting in Ac-D-Nal-D-4-CI-Phe-D-Pal-L-Ser-L-Tyr-diEt-hArg-L-Leu-diEt-hArg-L-Pro-D-Ala-NH2 with a molecular weight of 1570.4 (anhydrous free base).
Molecular formula: C80H113N18O13Cl. xCH3CO2H. yH2O, hydrated salt where 2 ≤ x ≤ 3 and y ≤ 10.

Chemical structure.


CAS number.

The CAS Registry numbers are 124904-93-4 (free base); 129311-55-3 (acetate).

7 Medicine Schedule (Poisons Standard)

Prescription Only Medicine (Schedule 4).

Summary Table of Changes