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QuickView for Bicalutamide (compound)

Summary
General Info

PubChem

PubChem Compound 2375

PubChem Compound 2375

Name:	bicalutamide
PubChem Compound ID:	2375
Molecular formula:	C₁₈H₁₄F₄N₂O₄S
Molecular weight:	430.374 g/mol
Synonyms:	NSC722665; ICI-176334; Raffolutil; LS-119125; Bicalutamide; Casodex

DrugBank

Identification

Name:	bicalutamide
Name (isomeric):	DB01128
Drug Type:	small molecule
Brand:	Casodex
Category:	Androgen Antagonists, Antineoplastic Agents
CAS number:	90357-06-5

Pharmacology

Indication:	For treatment (together with surgery or LHRH analogue) of advanced prostatic cancer.
Pharmacology:	Bicalutamide is an antineoplastic hormonal agent primarily used in the treatment of prostate cancer. Bicalutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). Consequently, Bicalutamide blocks the action of androgens of adrenal and testicular origin whic... show more » Bicalutamide is an antineoplastic hormonal agent primarily used in the treatment of prostate cancer. Bicalutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). Consequently, Bicalutamide blocks the action of androgens of adrenal and testicular origin which stimulate the growth of normal and malignant prostatic tissue. Prostate cancer is mostly androgen-dependent and can be treated with surgical or chemical castration. To date, antiandrogen monotherapy has not consistently been shown to be equivalent to castration. show less «
Mechanism of Action:	Bicalutamide competes with androgen for the binding of androgen receptors, consequently blocking the action of androgens of adrenal and testicular origin which stimulate the growth of normal and malignant prostatic tissue.
Absorption:	Bicalutamide is well-absorbed following oral administration, although the absolute bioavailability is unknown.
Protein binding:	96%
Biotransformation:	Bicalutamide undergoes stereo specific metabolism. The S (inactive) isomer is metabolized primarily by glucuronidation. The R (active) isomer also undergoes glucuronidation but is predominantly oxidized to an inactive metabolite followed by glucuronidation.
Half Life:	5.9 days
Clearance:	Apparent oral cl=0.32 L/h [Normal Males]
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

Take without regard to meals, at the same time everyday.

Drug interaction:

Eplerenone	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of eplerenone. A lower starting dose of eplerenone (25 mg once daily) is recommended in patients with hypertension who are also taking drugs that are moderate inhibitors of CYP3A4.
Tolvaptan	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of tolvaptan. This combination is contraindicated.
Colchicine	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of colchicine. Increase monitoring for colchicine-related toxicity when using such combinations. Use extra caution in patients with impaired renal and/or hepatic function.
Halofantrine	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of halofantrine. Extreme caution, with possibly increased monitoring of cardiac status (e.g., ECG), should be used with concurrent use of halofantrine with any moderate CYP3A4 inhibitor(s).
Everolimus	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of everolimus. Consider therapy modification. Recommendations regarding optimal management of this interaction vary according to specific indication and product used.

Eplerenone	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of eplerenone. A lower starting dose of eplerenone (25 mg once daily) is recommended in patients with hypertension who are also taking drugs that are moderate inhibitors of CYP3A4.
Tolvaptan	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of tolvaptan. This combination is contraindicated.
Colchicine	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of colchicine. Increase monitoring for colchicine-related toxicity when using such combinations. Use extra caution in patients with impaired renal and/or hepatic function.
Halofantrine	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of halofantrine. Extreme caution, with possibly increased monitoring of cardiac status (e.g., ECG), should be used with concurrent use of halofantrine with any moderate CYP3A4 inhibitor(s).
Everolimus	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of everolimus. Consider therapy modification. Recommendations regarding optimal management of this interaction vary according to specific indication and product used.
Ranolazine	CYP3A4 inhibitors like ranolazine may increase the serum concentration of ranolazine. Consider therapy modification.
Budesonide	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of budesonide. The clinical significance of this interaction is greater for oral budesonide than for orally inhaled budesonide. Consider reducing the oral budesonide dose when used together with a CYP3A4 inhibitor.
Lurasidone	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of lurasidone. Limit adult lurasidone dose to 40 mg/day in patients receiving a moderate CYP3A4 inhibitor.
Fentanyl	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of fentanyl. The risk of prolonged adverse effects, including potentially fatal respiratory depression is increased. Consider therapy modification.

Targets

Androgen receptor

Enzymes

Cytochrome P450 3A4

Cytochrome P450 2C19

Cytochrome P450 2C9

Cytochrome P450 2D6