Source: FDA, National Drug Code (US) Revision Year: 2020
PEMAZYRE is indicated for the treatment of adults with previously treated, unresectable locally advanced or metastatic cholangiocarcinoma with a fibroblast growth factor receptor 2 (FGFR2) fusion or other rearrangement as detected by an FDA-approved test [see Dosage and Administration (2.1)].
This indication is approved under accelerated approval based on overall response rate and duration of response [see Clinical Studies (14.1)]. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial(s).
Select patients for the treatment of locally advanced or metastatic cholangiocarcinoma with PEMAZYRE based on the presence of an FGFR2 fusion or rearrangement as detected by an FDA-approved test [see Clinical Studies (14.1)].
The recommended dosage of PEMAZYRE is 13.5 mg orally once daily for 14 consecutive days followed by 7 days off therapy, in 21-day cycles. Continue treatment until disease progression or unacceptable toxicity occurs.
Take PEMAZYRE with or without food at approximately the same time every day [see Clinical Pharmacology (12.3)].
Swallow tablets whole. Do not crush, chew, split, or dissolve tablets.
If the patient misses a dose of PEMAZYRE by 4 or more hours or if vomiting occurs, resume dosing with the next scheduled dose.
The recommended dose reductions for adverse reactions are provided in Table 1.
Table 1. Recommended Dose Reductions for PEMAZYRE for Adverse Reactions:
| Dose Reduction | >Recommended Dosage |
|---|---|
| First | 9 mg once daily for first 14 days of each 21-day cycle |
| Second* | 4.5 mg once daily for first 14 days of each 21-day cycle |
* Permanently discontinue PEMAZYRE if unable to tolerate 4.5 mg once daily.
The recommended dosage modifications for adverse reactions are provided in Table 2.
Table 2. Recommended Dosage Modifications for PEMAZYRE Adverse Reactions:
| Adverse Reaction | Severity* | PEMAZYRE Dosage Modification |
|---|---|---|
| Retinal Pigment Epithelial Detachment (RPED) [see Warnings and Precautions (5.1)] | RPED | • If asymptomatic and stable on serial examination, continue PEMAZYRE. • If symptomatic or worsening on serial examination, withhold PEMAZYRE.•• If asymptomatic and improved on subsequent examination, resume PEMAZYRE at a lower dose •• If symptoms persist or examination does not improve, consider permanent discontinuation of PEMAZYRE, based on clinical status. |
| Hyperphosphatemia [see Warnings and Precautions (5.2)] | Serum phosphate >7 mg/dL - ≤10 mg/dL | • Initiate phosphate lowering therapy and monitor serum phosphate weekly. • Withhold PEMAZYRE if levels are not <7 mg/dL within 2 weeks of starting phosphate lowering therapy. • Resume PEMAZYRE at the same dose when phosphate levels are <7 mg/dL for first occurrence; resume at a lower dose level for subsequent recurrences. |
| Serum phosphate >10 mg/dL | • Initiate phosphate lowering therapy and monitor serum phosphate weekly. • Withhold PEMAZYRE if levels are not ≤10 mg/dL within 1 week after starting phosphate lowering therapy. • Resume PEMAZYRE at the next lower dose level when phosphate levels are <7 mg/dL. • Permanently discontinue PEMAZYRE for recurrence of serum phosphate >10mg/dL following 2 dose reductions. | |
| Other Adverse Reactions | Grade 3 | • Withhold PEMAZYRE until resolves to Grade 1 or baseline. • Resume PEMAZYRE at next lower dose if resolves within 2 weeks. • Permanently discontinue PEMAZYRE if does not resolve within 2 weeks. • Permanently discontinue PEMAZYRE for recurrent Grade 3 after 2 dose reductions. |
| Grade 4 | • Permanently discontinue PEMAZYRE. |
* Severity as defined by National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) version 4 .03.
Avoid concomitant use of strong and moderate CYP3A inhibitors with PEMAZYRE. If concomitant use with a strong or moderate CYP3A inhibitor cannot be avoided:
If concomitant use of a strong or moderate CYP3A inhibitor is discontinued, increase the PEMAZYRE dose (after 3 plasma half-lives of the CYP3A inhibitor) to the dose that was used before starting the strong inhibitor [see Clinical Pharmacology (12.3)].
Store PEMAZYRE tablets at room temperature 20°C‑25°C (68°F‑77°F); excursions permitted to 15°C‑30°C (59°F‑86°F).
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