FOLLISTIM AQ
Clinical safety rating
cautionComprehensive clinical and safety monograph for FOLLISTIM AQ (FOLLISTIM AQ).
Comprehensive clinical and safety monograph for FOLLISTIM AQ (FOLLISTIM AQ).
Ovulation induction in anovulatory womenDevelopment of multiple follicles in assisted reproductive technologies (ART)Controlled ovarian hyperstimulation for in vitro fertilization (IVF)Hypogonadotropic hypogonadism (off-label)
Recombinant human follicle-stimulating hormone (FSH) that binds to FSH receptors on granulosa cells in the ovary, stimulating follicular growth and maturation via activation of adenylyl cyclase and increased cAMP production.
| Metabolism | Metabolized via hepatic and renal pathways; exact enzymes not specified. |
| Excretion | Primarily renal (90%), with intact follitropin alfa/beta and metabolites excreted in urine; biliary/fecal excretion minimal (<10%). |
| Half-life | Terminal elimination half-life approximately 24-36 hours (subcutaneous route); clinical context supports daily dosing due to sustained follicular stimulation. |
| Protein binding | Approximately 60-70% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Approximately 0.5-1.0 L/kg, indicating distribution primarily into extracellular fluid; limited tissue binding. |
| Bioavailability | Subcutaneous injection: approximately 70% (relative to IV); intramuscular injection: approximately 60-70%. |
| Onset of Action | Subcutaneous: follicular recruitment begins within 24-48 hours; peak serum estradiol rise by day 5-7 of treatment. |
| Duration of Action | Subcutaneous: therapeutic effect lasts 24-48 hours after last dose, supporting daily administration for follicular development. |
| Molecular Weight | Follitropin alfa is a glycoprotein with a molecular weight of approximately 30,000 Da (30 kDa). |
75 to 300 IU subcutaneously once daily for 8 to 14 days, adjusted based on follicular response; maximum daily dose 450 IU and total duration not exceeding 14 days per cycle.
| Dosage form | INJECTABLE |
| Renal impairment | No formal guidelines; use with caution in moderate to severe renal impairment (eGFR <30 mL/min/1.73 m²) due to limited data; consider lower starting doses based on clinical response. |
| Liver impairment | No formal guidelines; use with caution in Child-Pugh class B or C cirrhosis due to potential altered metabolism; monitor response and consider dose reduction. |
| Pediatric use | Not FDA-approved for pediatric use; limited off-label data for anovulatory disorders: start at 75 IU subcutaneously once daily, adjusted per response, based on body weight (1.5-3 IU/kg/day) with careful monitoring. |
| Geriatric use | Not indicated for geriatric use in fertility; no specific dosing recommendations; consider increased risk of adverse events if used off-label; monitor closely. |
| 1st trimester | Follistim AQ is not indicated for use during pregnancy. Inadvertent use during early pregnancy is unlikely to cause harm, but there are no adequate and well-controlled studies. Use only if clearly needed. |
| 2nd trimester | Not indicated for use during pregnancy. No data available for second trimester. |
| 3rd trimester | Not indicated for use during pregnancy. No data available for third trimester. |
Clinical note
Comprehensive clinical and safety monograph for FOLLISTIM AQ (FOLLISTIM AQ).
| Placental transfer | Follitropin alfa is a glycoprotein hormone with high molecular weight; placental transfer is expected to be minimal or negligible based on its size and structure. No specific studies on placental transfer in humans. |
| Breastfeeding | Follistim AQ is not indicated for use during breastfeeding. It is unknown whether follitropin alfa is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when administered to a nursing woman. Due to the indication (ovulation induction or controlled ovarian stimulation), use during breastfeeding is unlikely. |
| Lactation Rating | L5 |
| Teratogenic Risk | Follistim Aq (follitropin beta) is classified as Pregnancy Category X. It is contraindicated in pregnant women due to the risk of ovarian hyperstimulation syndrome and potential fetal harm. First trimester: No adequate human data, but animal studies show embryotoxicity. Second and third trimesters: Not indicated for use; may cause fetal harm if inadvertently administered during early pregnancy. |
| Fetal Monitoring | Monitor for signs of ovarian hyperstimulation syndrome (OHSS), including pelvic pain, distension, nausea, vomiting, and weight gain. Perform serial ultrasounds to assess ovarian size and follicle development. Monitor estradiol levels to reduce risk of OHSS. Fetal monitoring includes ultrasonography for multiple gestation and ectopic pregnancy. |
| Fertility Effects | Follitropin beta stimulates multiple follicular development, used for ovulation induction and controlled ovarian stimulation. It increases the risk of multiple gestation (twins, triplets) and OHSS. No evidence of long-term impairment of fertility, but ovarian hyperstimulation may temporarily affect reproductive function. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to follitropin alfa or any excipientsHigh levels of FSH indicating primary ovarian failureUncontrolled thyroid or adrenal dysfunctionSex hormone dependent tumors (e.g., ovarian, breast, uterine, pituitary or hypothalamic tumors)Ovarian enlargement or cyst not due to polycystic ovary syndromeAbnormal uterine bleeding of undetermined originPregnancy or lactation
| Precautions | Ovarian hyperstimulation syndrome (OHSS), Ovarian torsion, Multiple pregnancies, Pulmonary embolism, Ovarian enlargement, Ectopic pregnancy, Congenital malformations |
| Food/Dietary | No significant food interactions. Maintain a healthy diet; no specific restrictions. |
| Clinical Pearls | Administer subcutaneously; rotate injection sites to avoid lipodystrophy. Do not administer if solution contains particles or discoloration. Use the lowest effective dose to minimize risk of ovarian hyperstimulation syndrome (OHSS). Monitor estradiol levels and ultrasound for follicular development. Discontinue if pregnancy occurs. Store in refrigerator at 2-8°C; do not freeze. Protect from light. |
| Patient Advice | Inject exactly as prescribed; do not change dose without consulting your doctor. · Rotate injection sites (abdomen, thigh) to prevent lumps or skin reactions. · Report severe pelvic pain, nausea, vomiting, or rapid weight gain (signs of OHSS) immediately. · Avoid pregnancy during treatment; use barrier contraception until advised by your doctor. · Do not shake the cartridge; gently swirl to mix. · Store in the refrigerator; do not freeze. If unrefrigerated, use within 28 days at room temperature (≤25°C). · Discard any unused solution after the course of treatment. |
Loading safety data…