Tibolone

GENITO URINARY SYSTEM AND SEX HORMONES

Key facts

Tibolone is a drug catalogued in DrugCentral. It was first approved by the YEAR INTRODUCED in 1988. DrugCentral lists 8 molecular targets, including PGR, SLC6A4 and Ar. Recorded indications include Postmenopausal osteoporosis.

• Molecular targets: PGR, SLC6A4, Ar and ESR1 (8 listed in DrugCentral).
• Indications: Postmenopausal osteoporosis.
• ATC code: G03CX01 (Other estrogens).
• Molecular formula: C21H28O2; molecular weight 312.45 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Postmenopausal osteoporosis

Mechanism & targets

Molecular targets (8)

Target	Gene	Action	Activity
Progesterone receptor	PGR	unknown	Ki 7.54
Sodium-dependent serotonin transporter	SLC6A4	unknown	Ki 7.32
Androgen receptor	Ar	unknown	Ki 7.12
Estrogen receptor	ESR1	unknown	Ki 6.91
Cytochrome P450 2C19	CYP2C19	unknown	IC50 5.52
Progesterone receptor	PGR	unknown	—
Steryl-sulfatase	STS	unknown	—
Androgen receptor	AR	unknown	—

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1988-01-01	YEAR INTRODUCED	—	—

ATC classification

ATC code	Therapeutic hierarchy
G03CX01	GENITO URINARY SYSTEM AND SEX HORMONES › SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM › ESTROGENS › Other estrogens

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Breast cancer stage II	23.8
Infusion site reaction	23.1

Chemical structure

• Molecular formula: C₂₁H₂₈O₂
• Molecular weight: 312.45 g/mol
• CAS number: 5630-53-5
• InChIKey: WZDGZWOAQTVYBX-XOINTXKNSA-N
• PubChem CID: 444008

C[C@@H]1CC2=C(CCC(=O)C2)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@]3(O)C#C)[C@H]12

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Tibolone used for?

DrugCentral lists the following indications for Tibolone: Postmenopausal osteoporosis.

How does Tibolone work?

Its molecular targets in DrugCentral include PGR, SLC6A4, Ar and ESR1.

When was Tibolone first approved?

Tibolone was first approved by the YEAR INTRODUCED in 1988.

What is the chemical formula of Tibolone?

Tibolone has the molecular formula C21H28O2 and a molecular weight of 312.45 g/mol.

Sources

• DrugCentral drug card 2655 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL2103774 — compound record and bioactivity
• PubChem CID 444008 — chemical identifiers
• DrugBank DB09070 — drug record
• FDA UNII FF9X0205V2 — substance identity
• UniProt P31645 (SLC6A4) — target protein
• UniProt P03372 (ESR1) — target protein
• UniProt P33261 (CYP2C19) — target protein
• UniProt P06401 (PGR) — target protein
• UniProt P08842 (STS) — target protein
• UniProt P10275 (AR) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.