GONAL-F RFF
Clinical safety rating: caution
Comprehensive clinical and safety monograph for GONAL-F RFF (GONAL-F RFF).
Recombinant human follicle-stimulating hormone (FSH) that binds to FSH receptors on ovarian granulosa cells and testicular Sertoli cells, stimulating follicular growth and maturation and spermatogenesis.
| Metabolism | Primarily hepatic via proteolytic degradation and renal clearance |
| Excretion | Renal excretion: approximately 70% of the dose is eliminated in urine as intact hormone and metabolites; fecal excretion is negligible (<5%). |
| Half-life | Terminal elimination half-life: approximately 24-30 hours (range 24-36 h) following subcutaneous administration; supports once-daily dosing regimen. |
| Protein binding | Approximately 95% bound to plasma proteins, primarily albumin and sex hormone-binding globulin (SHBG). |
| Volume of Distribution | Volume of distribution: 6-10 L/kg, indicating extensive distribution into extracellular fluid and tissues (e.g., ovaries). |
| Bioavailability | Subcutaneous: approximately 70-80% (relative to intravenous administration); intramuscular: 100% (absolute bioavailability for Gonal-f RFF not explicitly reported, but similar to follitropin alfa). |
| Onset of Action | Subcutaneous: follicular growth (increase in estradiol levels) detectable within 24-48 hours; maximal response occurs after 5-7 days of daily dosing. |
| Duration of Action | Subcutaneous: effects on follicular development persist for up to 7-10 days after discontinuation; daily dosing required to maintain steady-state concentrations. |
Subcutaneous injection, initially 75-150 IU once daily for 5-7 days for ovulation induction. For controlled ovarian hyperstimulation, 75-300 IU once daily starting day 2 or 3 of cycle. Dose adjusted based on response.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment provided by manufacturer. GFR <30 mL/min: use with caution due to limited data. |
| Liver impairment | No specific dose adjustment provided by manufacturer. Child-Pugh Class C: use with caution; no established guidelines. |
| Pediatric use | Not indicated for use in pediatric patients. Safety and efficacy not established. |
| Geriatric use | Not indicated for use in geriatric patients. Safety and efficacy not established. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for GONAL-F RFF (GONAL-F RFF).
| Breastfeeding | No human data; M/P ratio unknown. Excretion in breast milk unknown; caution advised due to potential for serious adverse effects in infant. |
| Teratogenic Risk | Fetal risk cannot be ruled out. Category X: contraindicated in pregnancy due to risk of multiple gestation and ectopic pregnancy; no systematic evidence of teratogenicity but animal studies show post-implantation loss and fetal abnormalities at high doses. |
| Fetal Monitoring |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to FSH or any excipients","High levels of FSH indicating primary gonadal failure","Uncontrolled non-gonadal endocrinopathies (thyroid, adrenal, pituitary)","Sex hormone dependent tumors (ovarian, breast, uterus, testis, hypothalamus, pituitary)","Abnormal uterine bleeding of undetermined origin","Pregnancy and lactation"]
| Precautions | ["Ovarian hyperstimulation syndrome (OHSS)","Ovarian torsion","Multiple pregnancy","Pulmonary embolism and thromboembolic events","Ovarian enlargement","Ectopic pregnancy","Congenital malformations (risk similar to general population)"] |
Loading safety data…
| Monitor ovarian response via ultrasound and serum estradiol levels; assess for ovarian hyperstimulation syndrome (OHSS); monitor progesterone levels for luteal support. |
| Fertility Effects | Induces ovulation and follicular development; risk of multiple gestation; may cause ovarian hyperstimulation syndrome; utilized in assisted reproductive technology. |