BILDYOS
Clinical safety rating: caution
Comprehensive clinical and safety monograph for BILDYOS (BILDYOS).
BILDYOS (pemigatinib) is a selective, potent, oral inhibitor of fibroblast growth factor receptor (FGFR) 1, 2, and 3. It binds to the ATP-binding pocket of FGFR kinases, inhibiting autophosphorylation and downstream signaling, thereby reducing proliferation and survival of tumor cells with FGFR alterations.
| Metabolism | Primarily metabolized by cytochrome P450 (CYP) 3A4; minor contributions from CYP2C9 and CYP3A5. |
| Excretion | Primarily biliary/fecal (unchanged drug and metabolites), approximately 90%; renal excretion accounts for less than 10% as unchanged drug and conjugates. |
| Half-life | Approximately 24 hours at steady state; supports once-daily dosing. |
| Protein binding | >99% bound to human serum albumin. |
| Volume of Distribution | 12-15 L/kg, indicating extensive extravascular distribution. |
| Bioavailability | Approximately 70% after oral administration; absorption is reduced by food (high-fat meal decreases Cmax and AUC by ~50%). |
| Onset of Action | Oral: 2-4 hours for detectable serum levels; clinical effect onset within 24 hours for bile acid synthesis suppression. |
| Duration of Action | Approximately 24 hours, maintaining bile acid synthesis suppression over a 24-hour dosing interval. |
| Molecular Weight | 450.55 |
Adults: 20 mg orally once daily.
| Dosage form | INJECTABLE |
| Renal impairment | eGFR ≥30 mL/min: no adjustment. eGFR <30 mL/min: not recommended. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B or C: not recommended. |
| Pediatric use | Safety and efficacy not established; no recommended dose. |
| Geriatric use | No specific adjustment; use with caution due to age-related renal decline. |
| 1st trimester | Animal studies have shown teratogenic effects; human data insufficient. Use only if potential benefit justifies potential risk. |
| 2nd trimester | May cause fetal harm based on animal studies; avoid unless no safer alternative. |
| 3rd trimester | Risk of neonatal complications; use only if clearly needed and maternal benefit outweighs fetal risk. |
Clinical note
Comprehensive clinical and safety monograph for BILDYOS (BILDYOS).
| Placental transfer | Crosses placenta in animal models; human data limited but suggests significant transfer. |
| Breastfeeding | Excreted in human milk in small amounts; risk of adverse effects in nursing infants unknown. Caution advised. |
| Lactation Rating |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to drug or excipientsSevere hepatic impairment
| Precautions | Retinal pigment epithelial detachment (RPED), dry eye, keratitis, hyperphosphatemia leading to soft tissue mineralization (including cutaneous and vascular calcification), embryo-fetal toxicity, and cataracts. |
| Food/Dietary | No significant food interactions. Grapefruit juice has no known interaction. Alcohol should be limited due to potential hepatotoxicity. |
| Clinical Pearls |
Loading safety data…
| L3 (Moderately Safe) |
| Teratogenic Risk | First trimester: data insufficient; animal studies not adequate. Second trimester: no specific risks known. Third trimester: no specific risks known. Overall, avoid unless benefit outweighs risk. |
| Fetal Monitoring | Monitor maternal LFTs, renal function, and blood counts monthly. For fetus, serial growth ultrasounds due to limited safety data. |
| Fertility Effects | No human studies; animal data show no impairment of fertility at therapeutic doses. |
| BILDYOS is a biosimilar to adalimumab; ensure patient has no active infections before starting. Do not switch between biosimilars without prescriber authorization. Monitor for injection site reactions and new or worsening neurological symptoms. Live vaccines are contraindicated during therapy. |
| Patient Advice | Store in refrigerator at 2°C to 8°C; do not freeze or shake. · Inject subcutaneously as directed; rotate injection sites. · Report signs of infection (fever, cough, painful urination) immediately. · Avoid live vaccines (e.g., MMR, nasal flu) during treatment. · Seek urgent care if symptoms of allergic reaction occur. |