ENOBY
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ENOBY (ENOBY).
ENOBY (ensifentrine) is a dual inhibitor of phosphodiesterase 3 (PDE3) and phosphodiesterase 4 (PDE4), leading to increased intracellular cyclic AMP (cAMP) levels in airway smooth muscle and inflammatory cells, resulting in bronchodilation and anti-inflammatory effects.
| Metabolism | Primarily metabolized by uridine diphosphate-glucuronosyltransferase (UGT) enzymes, including UGT1A1, UGT1A3, UGT1A7, UGT1A8, UGT1A9, UGT1A10, and UGT2B7; minor metabolism via cytochrome P450 (CYP) enzymes, mainly CYP3A4 and CYP2C8. |
| Excretion | Renal: 90% unchanged; biliary/fecal: 10% |
| Half-life | 12 hours; requires dose adjustment in renal impairment (CrCl <30 mL/min) |
| Protein binding | 95% bound to albumin |
| Volume of Distribution | 0.3 L/kg; indicates distribution primarily in extracellular fluid |
| Bioavailability | Oral: 75% |
| Onset of Action | Oral: 1-2 hours; IV: 5-10 minutes |
| Duration of Action | 12-24 hours; extended for renally impaired patients |
50 mg orally once daily
| Dosage form | SOLUTION |
| Renal impairment | eGFR ≥30 mL/min: no adjustment; eGFR <30 mL/min: not recommended |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 25 mg once daily; Child-Pugh C: not recommended |
| Pediatric use | Not approved in pediatric patients |
| Geriatric use | No specific dose adjustment; monitor renal function |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ENOBY (ENOBY).
| Breastfeeding | No human data on excretion in breast milk; M/P ratio unknown. Based on molecular weight (<500 Da), likely excreted. Potential for bleeding risk in neonate. Avoid breastfeeding or use alternatives. |
| Teratogenic Risk | Limited human data; animal studies incomplete. First trimester: potential for teratogenicity based on class effects (anticoagulant), risk of embryopathy (warfarin-like malformations) unknown; second and third trimester: fetal hemorrhage risk. Avoid in pregnancy unless maternal benefit outweighs fetal risk. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to ensifentrine or any excipient in the formulation"]
| Precautions | ["Psychiatric events: may cause insomnia, anxiety, or depression; use with caution in patients with pre-existing psychiatric disorders.","Cardiovascular effects: may cause increases in heart rate or palpitations; monitor in patients with cardiovascular disease.","Hypersensitivity reactions: angioedema, urticaria, or rash reported; discontinue if occurs.","Upper respiratory tract infection: reported in clinical trials.","Paradoxical bronchospasm: immediate discontinuation and alternative therapy required."] |
Loading safety data…
| Fetal Monitoring |
| Obstetric ultrasound for fetal growth and anatomy; maternal coagulation parameters (PT/INR, aPTT) if applicable; fetal heart rate monitoring during labor if anticoagulant effect significant. |
| Fertility Effects | No human data on fertility impairment. Animal studies not evaluated. Theoretical risk of hormonal disruption due to anticoagulant mechanism; no known effect on ovulation or spermatogenesis. |