Tafamidisum

Tafamidisum Uses, Dosage, Side Effects, Food Interaction and all others data.

Tafamidisum and tafamidis meglumine (FX-1006A) are benzoxazole derivatives developed by FoldRX. Tafamidisum is structurally similar to diflusinal.

Tafamidisum was granted an EMA market authorisation on 16 November 2011 and FDA approval on 3 May 2019.

Tafamidisum stabilizes transthyretin tetramers, reducing the amount of monomers available for amyloidogenesis. It has a long duration of action as it is given once daily, and a wide therapeutic window.

Tafamidisum
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Tafamidisum
Availability	Prescription only
Generic	Tafamidis
Tafamidis Other Names	Tafamidis, Tafamidisum
Related Drugs	Vyndamax, Onpattro, Vyndaqel, Amvuttra, patisiran
Type
Formula	C₁₄H₇Cl₂NO₃
Weight	Average: 308.116 Monoisotopic: 306.980298509
Protein binding	Tafamidis 99.9% protein bound in plasma, mostly to transthyretin.
Groups	Approved, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Tafamidisum is a medication used to treat transthyretin-mediated amyloidosis.

Tafamidisum is indicated to treat cardiomyopathy of wild type or hereditary transthyretin-mediated amyloidosis in adults.

Tafamidisum is also used to associated treatment for these conditions: Cardiomyopathy

How Tafamidisum works

Genetic mutations or natural misfolding of transthyretin destabalizes transthyretin tetramers, leading to their dissociation and aggregation in tissues, and disrupting the normal function of these tissues. Tafamidisum binds to transthyretin tetramers at the thyroxin binding sites, stabilizing the tetramer, reducing the availability of monomers for amyloidogenesis.

Toxicity

Data regarding overdoses of tafamidis are not readily available. In a clinical trial, some patients were given up to 6 times the normal dose with one reported case of mild hordeolum.

Food Interaction

Take with or without food.

Tafamidisum Drug Interaction

Moderate: bumetanide, rosuvastatin, acetaminophenUnknown: risedronate, aspirin, suvorexant, diphenhydramine, tadalafil, methylcellulose, loratadine, sulfamethoxazole / trimethoprim, colchicine, apixaban, ethanol, ferrous sulfate, metoprolol, tramadol, ascorbic acid, cholecalciferol, metolazone

Tafamidisum Disease Interaction

Moderate: hypothyroidism, liver disease

Volume of Distribution

The apparent volume of distribution at steady state is 18.5L.

Elimination Route

Tafamidisum reaches a C_max of 1430.93ng/mL with a T_max of 1.75h fasted and 4h fed. The AUC of tafamidis is 47,864.31ng*h/mL.

Half Life

The half life of tafamidis is 49h.

Clearance

The oral clearance of tafamidis is 0.263L/h. The apparent total clearance is 0.44L/h.

Elimination Route

A 20mg oral dose of tafamidis is approximately 59% recovered in the feces, largely as unchanged drug. Approximately 22% of a 20mg oral dose is recovered in the urine, mostly as the glucuronide metabolite.