MYCAPSSA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for MYCAPSSA (MYCAPSSA).
Somatostatin analogue that inhibits growth hormone (GH), insulin-like growth factor 1 (IGF-1), and glucagon secretion by binding to somatostatin receptors (subtypes 2 and 5 predominantly).
| Metabolism | Primarily hepatic via CYP3A4; undergoes extensive first-pass metabolism. Excreted via bile and urine. |
| Excretion | Renal excretion accounts for approximately 50-60% of clearance, with the remainder primarily hepatic/biliary excretion (30-40%) and fecal elimination (10-20%). Unchanged drug in urine is minimal (<10%); most is excreted as metabolites. |
| Half-life | Terminal elimination half-life is approximately 11-13 hours in healthy volunteers, allowing for twice-daily dosing. In patients with moderate hepatic impairment, half-life may be prolonged, necessitating dose adjustment. |
| Protein binding | Approximately 90% bound to plasma proteins, primarily to alpha-1-acid glycoprotein and, to a lesser extent, albumin. |
| Volume of Distribution | Volume of distribution (Vd) is approximately 0.5-0.6 L/kg, indicating distribution primarily into extracellular fluid, with limited tissue penetration. |
| Bioavailability | Subcutaneous injection: Absolute bioavailability is approximately 90%. Oral bioavailability is negligible (<1%) and not clinically relevant. |
| Onset of Action | Subcutaneous injection: Peak concentrations occur at ~1-2 hours; clinical effects on growth hormone suppression are observed within 2-4 hours. |
| Duration of Action | Duration of growth hormone suppression is approximately 8-12 hours following a single subcutaneous dose, supporting twice-daily dosing. Clinical effects on symptoms of acromegaly are sustained with regular dosing. |
| Molecular Weight | 1019.3 |
40 mg subcutaneously twice daily.
| Dosage form | CAPSULE, DELAYED RELEASE |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment; not studied in severe renal impairment (CrCl <30 mL/min) or end-stage renal disease. |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh A and B); not studied in severe hepatic impairment (Child-Pugh C). |
| Pediatric use | Not established in pediatric patients. |
| Geriatric use | No specific dose adjustment; use with caution due to potential age-related renal or hepatic function decline. |
| 1st trimester | No adequate human studies; animal studies show no evidence of teratogenicity at clinically relevant doses. Use only if clearly needed. |
| 2nd trimester | No adequate human studies; potential risks unknown. Consider maternal benefit vs fetal risk. |
| 3rd trimester | No adequate human studies; potential risks unknown. Consider maternal benefit vs fetal risk. |
Clinical note
Comprehensive clinical and safety monograph for MYCAPSSA (MYCAPSSA).
| Placental transfer | Oligopeptide, expected to cross placenta to some degree based on molecular size; no data in humans. |
| Breastfeeding | It is not known whether octreotide is excreted in human milk. Caution is advised due to potential for growth inhibition or other adverse effects in the nursing infant. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to octreotide or any component of the formulation
| Precautions | Cholelithiasis (gallbladder sludge/stones), Hyperglycemia or hypoglycemia, Bradycardia, heart block, Hepatic impairment, Renal impairment, Pancreatitis, Hypothyroidism |
| Food/Dietary | Food reduces absorption of octreotide; therefore, take on an empty stomach (at least 1 hour before or 2 hours after meals). Avoid high-fat meals especially during dosing. There are no specific food restrictions beyond timing. |
| Clinical Pearls |
Loading safety data…
| Lactation Rating |
| L3 (Moderately Safe) |
| Teratogenic Risk | Insufficient human data; animal studies show fetal harm at 4 times human exposure. Embryolethality, skeletal anomalies, reduced fetal weight observed in rodents. Risk cannot be excluded; avoid use in pregnancy unless benefit outweighs risk. |
| Fetal Monitoring | Monitor maternal renal function, electrolytes, glucose; fetal ultrasound for growth if continued during pregnancy. |
| Fertility Effects | Reduced fertility in male rats at high doses; human data absent. |
| MYCAPSSA (octreotide) delayed-release capsules are used for acromegaly and neuroendocrine tumors. Administer on an empty stomach at least 1 hour before or 2 hours after meals. Do not crush or open capsules; swallow whole. Monitor for gallbladder abnormalities, bradycardia, hypoglycemia/hyperglycemia, and thyroid function. Dose adjustments may be needed in hepatic impairment. Concomitant use with cyclosporine may alter cyclosporine levels. |
| Patient Advice | Take capsules on an empty stomach, at least 1 hour before or 2 hours after a meal. · Swallow capsule whole; do not crush, chew, or open it. · If you miss a dose, skip it; do not double the next dose. · Report symptoms like gallstones (abdominal pain), slow heart rate, or blood sugar changes. · Avoid alcohol and high-fat meals as they may affect drug absorption. · Use effective contraception if of childbearing potential; tell your doctor if you are pregnant or breastfeeding. |