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Triptodur (triptorelin) extended-release injectable suspension

Summary about Triptodur

Triptodur is an injectable prescription medicine used for the treatment of children with central precocious puberty (CPP). It is administered as a single intramuscular (IM) injection just once every 24 weeks, making it the first FDA-approved medicine for CPP to offer once-every six-month dosing. Treatment with Triptodur does not require surgery.

The process of puberty starts in the brain with the creation of a hormone called gonadotropin-releasing hormone (GnRH). GnRH causes the pituitary gland — a small bean-shaped gland at the base of the brain — to release two more hormones called luteinizing hormone (LH) and follicle-stimulating hormone (FSH). LH and FSH are involved in the growth and development of female and male sexual characteristics.

Treatments for CPP weaken the effects of GnRH signaling on the pituitary gland, reducing the release of hormones that cause puberty. By stopping the signaling of these hormones, the puberty process will be delayed until the end of the treatment. The effect of Triptodur on pituitary and gonadal function is expected to disappear within six to twelve months after treatment is stopped.

Triptodur is effective in suppressing LH to prepubertal levels (≤5 IU/L):

  • In a phase III clinical trial, 93% of patients receiving Triptodur had their LH suppressed to prepubertal levels at month six, and 98% of patients maintained these levels at 12 months.
  • Triptodur was also found to be safe and well tolerated with no unexpected side effects

Triptodur must be administered under the supervision of a physician. It is important to stick to the dosing schedule (one injection every 24 weeks) in order for the medicine to work. Do not miss or delay a scheduled dose.

Your child should have regular visits with his or her pediatrician or pediatric endocrinologist while undergoing treatment for CPP.

During your child’s treatment, a healthcare professional will perform regular exams and blood tests to check for signs of puberty, measure height and weight, and may take wrist X-rays to track bone growth.

The most common side effects of Triptodur include injection site reactions, menstrual (vaginal) bleeding, hot flush, headache, cough, and infections (bronchitis, gastroenteritis, influenza, nasopharyngitis, otitis externa, pharyngitis, sinusitis, and upper respiratory tract infection).

 

 

Triptodur (triptorelin)

Active Ingredient

Triptorelin

Administration Route

Intramuscular

Alcohol Warning

No data about interaction

Available Strength

For extended-release injectable suspension: 22.5 mg of triptorelin as a powder cake for reconstitution with the co-packaged 2 mL of diluent Sterile Water for Injection.

Breastfeeding Warning

A decision should be made to discontinue breastfeeding or discontinue the drug, taking into account the importance of the drug to the mother.

Excreted into human milk: Unknown
Excreted into animal milk: Data not available

There is a potential for serious adverse reactions in nursing infants.

Clinical Pharmacology

Pharmacodynamics

Following the first administration, there is a transient surge in circulating levels of LH, FSH, testosterone, and estradiol. After chronic and continuous administration, by 4 weeks after initiation of therapy, a sustained decrease in LH and FSH secretion and marked reduction in sex steroids are observed.

Pharmacokinetics

Absorption

After an initial intramuscular TRIPTODUR 22.5 mg injection and a second 22.5 mg intramuscular injection 24 weeks later in children 2 to 9 years old with CPP, triptorelin peaked 4 hours postdose with a geometric mean Cmax of 39.9 and 36.5 ng/mL, respectively. No apparent accumulation of triptorelin occurred after the second injection. Absorption occurred in two phases, a burst phase followed by a maintenance release phase. In children with CPP, following the burst phase after the first 22.5 mg injection, geometric mean serum triptorelin levels were 0.11, 0.17, 0.05 and 0.03 ng/mL at Months 1, 2, 3, and 6, respectively.

Distribution

There is no evidence that triptorelin, at clinically relevant concentrations, binds to plasma proteins.

Elimination

Metabolism

The metabolism of triptorelin in humans is unknown, but is unlikely to involve hepatic microsomal enzymes (cytochrome P450). Thus far no metabolites of triptorelin have been identified. Pharmacokinetic data suggest that C-terminal fragments produced by tissue degradation are either completely degraded in the tissues, or rapidly degraded in plasma, or cleared by the kidneys.

Excretion

Triptorelin is eliminated by both the liver and the kidneys. Following intravenous administration of 0.5 mg triptorelin peptide to six healthy male volunteers with a creatinine clearance of 149.9 mL/min, 41.7% of the dose was excreted in urine as intact peptide with a total triptorelin clearance of 211.9 mL/min. This percentage increased to 62.3% in patients with liver disease who have a lower creatinine clearance (89.9 mL/min). It has also been observed that the nonrenal clearance of triptorelin (patient anuric, Clcreat = 0) was 76.2 mL/min, thus indicating that the nonrenal elimination of triptorelin is mainly dependent on the liver.

Specific Populations

Renal Impairment

After intravenous bolus injection of 0.5 mg triptorelin in adults, the two distribution half-lives were unaffected by renal impairment. However, renal insufficiency led to a decrease in total triptorelin clearance proportional to the decrease in creatinine clearance as well as increases in volume of distribution and consequently, an increase in the elimination half-life. Adult male subjects with moderate or severe renal impairment had approximately 2-fold higher exposure (AUC values) than young healthy adult males.

Hepatic Impairment

After intravenous bolus injection of 0.5 mg triptorelin in adults, the two distribution half-lives were unaffected by hepatic impairment. In adult males with hepatic insufficiency, triptorelin clearance was reduced and exposure (AUC) was increased 3.7-fold compared to young healthy adult males.

Cost

Approximate Retail Price according https://www.drugs.com/price-guide/triptodur

Intramuscular Powder For Injection, Extended Release:

  • 22.5 mg (1 powder for injection): $17,130.10

Dosage Form

Intramuscular Powder For Injection, Extended Release

Dose Schedule

Must only be administered by a healthcare provider.

The dosage of TRIPTODUR is 22.5 mg reconstituted with accompanying diluent (sterile water) 2 mL, and administered as a single intramuscular injection once every 24 weeks.

TRIPTODUR treatment should be discontinued at the appropriate age of onset of puberty at the discretion of the physician.

Monitoring

Monitor response to TRIPTODUR with LH levels after a GnRH or GnRH agonist stimulation test, basal LH, or serum concentration of sex steroid levels beginning 1 to 2 months following initiation of therapy, during therapy as necessary to confirm maintenance of efficacy, and with each subsequent dose.

Measure height (for calculation of growth rate) every 3-6 months and monitor bone age periodically.

Noncompliance with drug regimen or inadequate dosing may result in inadequate control of the pubertal process with gonadotropins and/or sex steroids increasing above prepubertal levels. If the dose of TRIPTODUR is not adequate switching to an alternative GnRH agonist for the treatment of CPP with the ability for dose adjustment may be necessary.

Drug Class

L02AE – Gonadotropin releasing hormone analogues

Drug Unit

mg

Food Warning

No formal drug-food, or drug-herb interaction studies were performed with Triptodur.

Included In
Health Insurance Plan

Find out more here: http://triptodur.com/care-program.php

Interacting Drugs

Drug-Drug Interactions

Results of in vitro studies show that drug-drug interactions with triptorelin are unlikely. However, in the absence of relevant data and as a precaution, hyperprolactinemic drugs should not be used concomitantly with triptorelin since hyperprolactinemia reduces the number of pituitary GnRH receptors.

Drug-Laboratory Test Interactions

Administration of TRIPTODUR results in suppression of the pituitary-gonadal system.

The effect of TRIPTODUR on pituitary and gonadal function is expected to disappear within six to twelve months after treatment discontinuation. Therefore, diagnostic tests of pituitary gonadotropic and gonadal functions conducted during treatment or after discontinuation of treatment may be affected.

Is Available Generically

Yes. There is a therapeutically equivalent version of Triptodur available under the generic name Triptorelin.

Is Proprietary

Yes

Label Details

https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208956s000lbl.pdf

Legal Status

Legal.

Is not subject to the Controlled Substances Act.

Manufacturer

Arbor Pharmaceuticals, Inc.

Maximum Intake

22.5 mg once in 24 weeks

Mechanism of Action

Triptorelin is a synthetic agonist analog of gonadotropin releasing hormone (GnRH). Animal studies comparing triptorelin to native GnRH found that triptorelin had 13 fold higher releasing activity for luteinizing hormone, and 21-fold higher releasing activity for follicle-stimulating hormone.

Non Proprietary Name

Triptorelin

Overdosage

There is no experience with overdosage in clinical trials of triptorelin. If overdosage occurs, therapy should be discontinued and appropriate supportive and symptomatic treatment administered.

Pregnancy Category


AU TGA pregnancy category D: Drugs which have caused, are suspected to have caused or may be expected to cause, an increased incidence of human fetal malformations or irreversible damage. These drugs may also have adverse pharmacological effects. Accompanying texts should be consulted for further details.US FDA pregnancy category X: Studies in animals or humans have demonstrated fetal abnormalities and/or there is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience, and the risks involved in use of the drug in pregnant women clearly outweigh potential benefits.

Pregnancy Warning

Use is contraindicated.

Animal studies during organogenesis showed embryo-fetal toxicities of pre-implantation loss, increased resorption, and reduced number of viable fetuses. There are no adequate or well-controlled studies in pregnant women. Expected treatment related hormonal changes increase the risk for pregnancy loss.

Prescribing Info

https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208956s000lbl.pdf

Prescription Status

Prescription drug

Proprietary Name

Triptodur

Related Drugs

Bicalutamide, Leuprolide, Triptorelin, Goserelin, Buserelin

RxCUI

1944385

Warning


Initial Rise of Gonadotropins and Sex Steroid Levels:
An increase in clinical signs and symptoms of puberty may be observed during the first 2­ 4 weeks of therapy since gonadotropins and sex steroids rise above baseline because of the initial stimulatory effect of the drug.Psychiatric events have been reported in patients taking GnRH agonists. Events include emotional lability, such as crying, irritability, impatience, anger, and aggression. Monitor for development or worsening of psychiatric symptoms.Convulsions have been observed in patients with or without a history of seizures, epilepsy, cerebrovascular disorders, central nervous system anomalies or tumors, and in patients on concomitant medications that have been associated with convulsions.

 

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