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What the FDA labels say about taking them together

Sapropterin and trimethoprim

Sapropterin's FDA label of August 26, 2024 names trimethoprim in its drug interactions section; the trimethoprim label PlainMeds reads does not name sapropterin. The sapropterin label: “Inhibitors of Folate Synthesis Clinical Impact In vitro and in vivo nonclinical data suggest that drugs that inhibit folate synthesis may decrease the bioavailability of endogenous BH4 by inhibiting the enzyme …”

Check it at the source: the sapropterin FDA label on DailyMed (effective August 26, 2024, BioMarin Pharmaceutical Inc.); the trimethoprim FDA label on DailyMed (effective January 26, 2024, Dr. Reddy's Labratories Inc.).

What does the sapropterin label say about trimethoprim?

Sapropterin label, drug interactions

Inhibitors of Folate Synthesis (e.g., methotrexate, valproic acid, phenobarbital, trimethoprim) Clinical Impact In vitro and in vivo nonclinical data suggest that drugs that inhibit folate synthesis may decrease the bioavailability of endogenous BH4 by inhibiting the enzyme dihydrofolate reductase, which is involved in the recycling (regeneration) of BH4. This reduction in net BH4 levels may increase Phe levels. Intervention Consider monitoring blood Phe levels more frequently during concomitant administration. An increased dosage of KUVAN may be necessary to achieve a biochemical response.

Source: FDA drug label (Kuvan), BioMarin Pharmaceutical Inc., effective August 26, 2024 (SPL set af38711e-8873-4790-a92d-4d583e23fb89), via openFDA; the full label on DailyMed

What does the trimethoprim label say about sapropterin?

Trimethoprim's label (effective January 26, 2024) does not name sapropterin in these sections. A label lists what its studies and reports found; it is not a complete list.

Source: FDA drug label (Trimethoprim), NDA018679 (Dr Reddys Labs Sa), as published by Dr. Reddy's Labratories Inc., effective January 26, 2024 (SPL set 73ccebc1-7412-2424-d62c-a5180ec52d81), via openFDA; the full label on DailyMed

These are the labels' own sentences. PlainMeds does not grade interactions; a pharmacist or prescriber can say what they mean for one person's medicines.

Both medicines on the record

9Sapropterin generic labelers
4Trimethoprim generic labelers
SapropterinTrimethoprim
Labeled forn/aBacterial infections, Urinary tract infections
Boxed warningNoNo
Pharmacy cost (NADAC)n/a$1.31 per tablet 100 mg tablet
Shortage nowNo current entryNo current entry

Source: FDA NDC Directory, CMS NADAC of October 7, 2026 and the FDA Drug Shortage Database (FDA files October 8, 2026)

What next?