Formulary
Tafamidis: Indications, Dosing, Side Effects and Interactions
Tafamidis is a transthyretin stabiliser which inhibits amyloid formation, thereby delaying the development of nerve and cardiac muscle damage caused by...
MedNext Academy | 3 min read
Tafamidis: Indications, Dosing, Side Effects and Interactions
Tafamidis is a transthyretin stabiliser which inhibits amyloid formation, thereby delaying the development of nerve and cardiac muscle damage caused by...
Drug action
Tafamidis is a transthyretin stabiliser which inhibits amyloid formation, thereby delaying the development of nerve and cardiac muscle damage caused by transthyretin amyloidosis.
Indications and dose
**Treatment of transthyretin amyloidosis in patients with stage 1 symptomatic polyneuropathy (ATTR-PN) [using 20 mg capsules] (initiated under specialist supervision)**
- **Adult** (By Mouth): 20 mg once daily.
**Treatment of wild-type transthyretin amyloidosis in patients with cardiomyopathy (ATTR-CM) [using 61 mg capsules] (initiated under specialist supervision),Treatment of hereditary transthyretin amyloidosis in patients with cardiomyopathy (ATTR-CM) [using 61 mg capsules] (initiated under specialist supervision)**
- **Adult** (By Mouth): Treatment of wild-type transthyretin amyloidosis in patients with cardiomyopathy (ATTR-CM) [using 61 mg capsules] (initiated under specialist supervision), Treatment of hereditary transthyretin amyloidosis in patients with cardiomyopathy (ATTR-CM) [using 61 mg capsules] (initiated under specialist supervision) 61 mg once daily.
Side effects
Common or very common Abdominal pain upper; diarrhoea; increased risk of infection Frequency not known Flatulence
Interactions
**Severe interactions:**
- Based on in vitro data, the maximal predicted changes in AUC of OAT1 and OAT3 substrates were determined to be less than 1.25 for the tafamidis 61 mg dose, therefore, inhibition of OAT1 or OAT3...
**Other interactions (7):**
- In a clinical study in healthy volunteers, 20 mg tafamidis meglumine did not induce or inhibit the cytochrome P450 enzyme CYP3A4.
- In vitro tafamidis inhibits the efflux transporter BCRP (breast cancer resistant protein) at the 61 mg/day tafamidis dose with IC50=1.16 M and may cause drug-drug interactions at clinically...
- In a clinical study in healthy participants, the exposure of the BCRP substrate rosuvastatin increased approximately 2-fold following multiple doses of 61 mg tafamidis daily dosing.
- Likewise, tafamidis inhibits the uptake transporters OAT1 and OAT3 (organic anion transporters) with IC50=2.9 M and IC50=2.36 M, respectively, and may cause drug-drug interactions at clinically...
- No interaction studies have been performed evaluating the effect of other medicinal products on tafamidis.
- Laboratory test abnormality Tafamidis may decrease serum concentrations of total thyroxine, without an accompanying change in free thyroxine (T4) or thyroid stimulating hormone (TSH).
Pregnancy
Avoid (toxicity in animal studies).
Breast feeding
Avoid-present in milk in animal studies.
Hepatic impairment
Manufacturer advises caution in severe impairment (no information available).
Medicinal forms
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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