FERTINEX
Clinical safety rating
cautionComprehensive clinical and safety monograph for FERTINEX (FERTINEX).
Comprehensive clinical and safety monograph for FERTINEX (FERTINEX).
Ovulation induction in anovulatory women with polycystic ovary syndrome (PCOS) who have failed to respond to clomiphene citrateControlled ovarian hyperstimulation for assisted reproductive technologies (ART) such as in vitro fertilization (IVF)Hypogonadotropic hypogonadism in men
Follitropin beta, a recombinant form of human follicle-stimulating hormone (FSH), binds to the FSH receptor on ovarian granulosa cells and testicular Sertoli cells, stimulating follicular development and maturation in women and spermatogenesis in men.
| Metabolism | Metabolized primarily via the liver and kidneys; exact enzymes not fully characterized, but involves hepatic degradation and renal excretion. |
| Excretion | Primarily renal excretion of unchanged drug (80-90% of administered dose), with the remainder excreted as metabolites in urine and feces. |
| Half-life | Terminal elimination half-life is approximately 24-36 hours in patients with normal renal function, supporting once-daily dosing. |
| Protein binding | Approximately 60-70% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Vd is approximately 0.3-0.5 L/kg, indicating distribution mainly into extracellular fluid. |
| Bioavailability | Subcutaneous: ~70% relative to intravenous; intramuscular: ~90% relative to intravenous. |
| Onset of Action | Subcutaneous injection: Clinical effect (increase in serum estradiol) observed within 5-7 days of daily dosing; intramuscular: similar onset. |
| Duration of Action | Duration of effect is 24-48 hours after single dose; repeated daily dosing required for follicular recruitment. |
| Molecular Weight | Approximately 31,000 Da (FSH is 31 kDa, derived from human menopausal gonadotropin) |
For ovulation induction: 75-150 IU subcutaneously or intramuscularly once daily for 7-12 days; for spermatogenesis: 75-150 IU subcutaneously or intramuscularly 3 times per week.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dosing guidelines; use with caution in severe renal impairment (CrCl <30 mL/min) due to limited data; consider reduced dose or extended interval. |
| Liver impairment | No specific dosing guidelines; use with caution in severe hepatic impairment (Child-Pugh class C) due to limited data; consider reduced dose. |
| Pediatric use | For delayed puberty (males): 75-150 IU subcutaneously or intramuscularly 3 times per week; adjust based on testosterone response. For cryptorchidism: 1000-1500 IU subcutaneously or intramuscularly 2-3 times per week for 4-6 weeks; not weight-based but age-adjusted. |
| Geriatric use | Elderly patients are not typically candidates for FERTINEX; no specific dose adjustments recommended due to lack of use; monitor for comorbidities and potential hypersensitivity. |
| 1st trimester | Fertinex (urofollitropin) is contraindicated in pregnancy. It is not indicated during the first trimester due to the risk of ovarian hyperstimulation syndrome and potential fetal harm. |
| 2nd trimester | Contraindicated during pregnancy. Second trimester exposure is not indicated; use is avoided. |
| 3rd trimester | Contraindicated during pregnancy. Third trimester exposure is not indicated; use is avoided. |
Clinical note
Comprehensive clinical and safety monograph for FERTINEX (FERTINEX).
| Placental transfer | Likely minimal due to high molecular weight and peptide nature; however, no specific human data on placental transfer are available. FSH is a large glycoprotein and is not expected to cross the placenta in significant amounts. |
| Breastfeeding | It is not known whether urofollitropin is excreted in human milk. Caution is advised, but due to the lack of data, use during breastfeeding is generally not recommended unless clearly necessary. |
| Lactation Rating | L3 (Moderately Safe, limited data) |
| Teratogenic Risk | Fertinex (urofollitropin) is associated with a Category X risk in pregnancy. Administration during pregnancy may cause fetal harm, including congenital malformations (neural tube defects, limb defects) and spontaneous abortion. Use is contraindicated in pregnant women. |
| Fetal Monitoring | Monitor ovarian response via transvaginal ultrasound and serum estradiol levels. Assess for ovarian hyperstimulation syndrome (OHSS). In case of pregnancy, monitor for multiple gestation and ectopic pregnancy. |
| Fertility Effects | Fertinex is used to induce ovulation in anovulatory women. It increases the risk of multiple pregnancy (twins, triplets) and may cause ovarian enlargement. Ovarian hyperstimulation syndrome is a potential adverse effect. |
■ FDA Black Box Warning
FERTINEX should only be used by physicians with expertise in infertility treatment. Ovarian hyperstimulation syndrome (OHSS) may occur, which can be severe and result in ovarian enlargement, pelvic pain, ascites, pleural effusion, and thromboembolic events. Multiple gestation increases the risk of adverse maternal and perinatal outcomes.
| Serious Effects |
PregnancyOvarian enlargement or cyst not due to polycystic ovary syndromeOvarian dysgenesis or premature ovarian failureSex hormone-dependent tumors (e.g., breast, uterus)Thyroid or adrenal insufficiency (uncontrolled)Hyperprolactinemia (uncontrolled)Primary ovarian failureUncontrolled non-gonadal endocrinopathies
| Precautions | Risk of ovarian hyperstimulation syndrome (OHSS), which may be severe and require hospitalization, Increased risk of multiple gestation (twins, triplets, etc.), Ovarian torsion reported, Potential for ovarian enlargement and cyst formation, Thromboembolic events, especially in patients with risk factors, Should not be used in patients with primary ovarian failure, uncontrolled thyroid/adrenal dysfunction, or sex hormone-dependent tumors |
| Food/Dietary | No specific food interactions. Maintain a balanced diet rich in folic acid (400-800 mcg/day) to reduce risk of neural tube defects. Avoid excessive alcohol and caffeine. |
| Clinical Pearls | FERTINEX (urofollitropin) is a purified FSH product used for ovulation induction. Monitor ovarian response via serum estradiol levels and transvaginal ultrasound to assess follicle size and number. Adjust dose based on response to minimize OHSS risk. Administer IM or SC after reconstitution. Use caution in patients at risk for thromboembolism. |
| Patient Advice | FERTINEX is a hormone injection given under the skin or into a muscle to help you ovulate. · You will need training on how to inject the medication and dispose of needles safely. · Common side effects include headache, bloating, and injection site reactions. · Seek immediate medical attention if you experience severe pelvic pain, sudden weight gain, or shortness of breath. · Avoid alcohol and limit caffeine intake during treatment. · Report any signs of ovarian hyperstimulation syndrome (OHSS) such as nausea, vomiting, or decreased urination. |
Loading safety data…