TRYNGOLZA (AUTOINJECTOR)
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TRYNGOLZA (AUTOINJECTOR) (TRYNGOLZA (AUTOINJECTOR)).
Selective inhibitor of protein kinase C theta (PKCθ), reducing T cell activation and cytokine production.
| Metabolism | Metabolized primarily by CYP3A4 and CYP2C8. |
| Excretion | Primarily eliminated via the reticuloendothelial system; no significant renal or biliary excretion. <1% excreted unchanged in urine. |
| Half-life | Terminal elimination half-life is approximately 21 days (range 14–28 days), consistent with slow clearance from plasma due to target-mediated drug disposition. |
| Protein binding | Approximately 99% bound; primarily to albumin and other plasma proteins. |
| Volume of Distribution | Vd is approximately 0.08 L/kg, indicating distribution primarily within the vascular space. |
| Bioavailability | Subcutaneous: Approximately 40–60% after autoinjector administration. |
| Onset of Action | Subcutaneous: Clinical effect (reduction in LDL-C) observed within 2–4 weeks after first dose. |
| Duration of Action | Duration of effect is approximately 2–4 weeks post-dose; repeat dosing every 2–4 weeks is required to maintain LDL-C reduction. |
0.5 mg subcutaneously once daily.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No dose adjustment required for hepatic impairment. |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | No specific dose adjustment recommended; use with caution due to potential comorbidities. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TRYNGOLZA (AUTOINJECTOR) (TRYNGOLZA (AUTOINJECTOR)).
| Breastfeeding | No data on excretion in human milk; M/P ratio not determined. Due to potential for serious adverse reactions in nursing infants, breastfeeding is not recommended during therapy and for 2 weeks after last dose. |
| Teratogenic Risk | Pregnancy Category X. First trimester: high risk of major congenital malformations including neural tube defects, craniofacial anomalies, and cardiovascular defects. Second and third trimesters: risk of oligohydramnios, fetal renal impairment, and skeletal abnormalities. Contraindicated in pregnancy. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Severe hypersensitivity to tryngolza or any excipients","Active serious infection"]
| Precautions | ["Increased risk of serious infections","Malignancies including lymphoma","Hepatotoxicity","Lipid abnormalities","Hypersensitivity reactions"] |
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| Fetal Monitoring |
| If inadvertent exposure occurs, monitor for oligohydramnios via ultrasound, fetal growth restriction, and fetal renal function. Perform pregnancy test before initiation and monthly during treatment. |
| Fertility Effects | May impair fertility in females based on animal studies showing ovarian and uterine effects. Reversible upon discontinuation. No human data available. |