darolutamide

medtigo

darolutamide

Brand Name :

Nubeqa

Synonyms :

darolutamide

Class :

Antiandrogens

Action and Spectrum

Actions and Spectrum:

darolutamide is indicated for the treatment of non-metastatic castration-resistant prostate cancer (nmCRPC) in adult men in combination with androgen deprivation therapy (ADT). It works by inhibiting the activity of the androgen receptor, which is a protein that plays a key role in the growth and progression of prostate cancer.

darolutamide has a broad spectrum of action, as it targets not only the androgen receptor but also other signalling pathways that are important for prostate cancer growth and progression. Its mechanism of action also includes inhibition of the intratumoral androgen biosynthesis and inhibition of the intratumoral androgen receptor signalling.

Dosing & Uses

Drug Interaction

Adverse Reaction

>10%:

Fatigue (16%)

AST increased (23%)

Bilirubin increased (16%)

1-10%:

Pain in extremity (6%)

Hemorrhage (1.4%)

Rash (1.8%)

Weight increased (2.1%)

<1%:

Bilirubin increased (0.1%)

Fatigue (0.6%)

Decreased appetite (0.2%)

Constipation (0.3%)

Black Box Warning

Black Box Warning:

It is essential to follow the dosage and administration instructions for the medication carefully.

Contraindication / Caution

Contraindication/Caution:

darolutamide should not be used in people hypersensitive to the drug itself.

Pregnancy / Lactation

Pregnancy consideration:

The drug is not safe for pregnant women.

Breastfeeding warnings:

The drug is not safe for females.

Pregnancy category:

Category A: well-controlled and Satisfactory studies do not show risk to the fetus in the first/later trimester.       
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.       
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.      
Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.       
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.       
Category N: No data is available for the drug under this category.

Pharmacology

Pharmacology

darolutamide is a highly selective androgen receptor antagonist that binds to the ligand-binding domain of the androgen receptor, preventing the binding of androgen and the activation of the androgen receptor. This blocks the downstream signalling events that promote prostate cancer cell growth, survival, and proliferation.

Pharmacodynamics:

The pharmacodynamics of darolutamide includes reducing the activity of the androgen receptor, inhibiting the growth and progression of prostate cancer cells, and improving outcomes in men with non-metastatic castration-resistant prostate cancer.

Pharmacokinetics:

Pharmacokinetics is the study of how a drug is absorbed, distributed, metabolized, and eliminated by the body. The pharmacokinetics of darolutamide can be described by the following parameters:

Absorption

darolutamide is well absorbed after oral administration, with peak plasma concentrations reached within 2 to 4 hours. Distribution

darolutamide is highly bound to plasma proteins, with a binding percentage of over 99%.

Metabolism

darolutamide is metabolized primarily by cytochrome P450 (CYP) 3A4 and CYP2C8 enzymes.

Elimination and excretion

The elimination half-life of darolutamide is about 40 hours, and it is primarily excreted in feces (about 80%) and urine (about 15%).

Adminstartion

Administration:

Take the medicine with food. Swallow as whole.

Patient Information Leaflet

Patient information leaflet

Generic Name: darolutamide

Pronounced: DAR-oh-LOO-tuh-mide

Why do we use darolutamide?

darolutamide is used to treat Nonmetastatic Castration-Resistant Prostate Cancer and Metastatic Hormone-Sensitive Prostate Cancer.

darolutamide

No data available for drug.

DRUG INTERACTION

darolutamide

&

darolutamide +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

darolutamide

No data available for drug.

DRUG INTERACTION

darolutamide

&

darolutamide +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

medtigo

darolutamide

Brand Name :

Synonyms :

Class :

Action and Spectrum

Dosing & Uses

Drug Interaction

Adverse Reaction

Black Box Warning

Contraindication / Caution

Pregnancy / Lactation

Pharmacology

Adminstartion

Patient Information Leaflet