Norethisterone

Progestin — GENITO URINARY SYSTEM AND SEX HORMONES

Key facts

Norethisterone is an ofp drug in the Progestin class catalogued in DrugCentral. It was first approved by the FDA in 1962. DrugCentral lists 9 molecular targets, including PGR, Esr1|Esr2 and PGR. Recorded indications include Acne vulgaris, Atrophic vaginitis, Atrophic vulva and Contraception.

• Approval status: ofp (first approved 1962 by the FDA).
• Drug class: Progestin.
• Molecular targets: PGR, Esr1|Esr2, PGR and SHBG (9 listed in DrugCentral).
• Indications: Acne vulgaris, Atrophic vaginitis, Atrophic vulva, Contraception and Controlled ovarian stimulation and others.
• ATC code: G03AA05 (Progestogens and estrogens, fixed combinations).
• Molecular formula: C20H26O2; molecular weight 298.43 g/mol.

Indications & contraindications

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

Indications (15)

• Acne vulgaris
• Atrophic vaginitis
• Atrophic vulva
• Contraception
• Controlled ovarian stimulation
• Dysfunctional uterine bleeding
• Endometriosis
• Female hypogonadism syndrome
• Menopausal flushing
• Menorrhagia
• Postmenopausal osteoporosis
• Primary ovarian failure
• Secondary physiologic amenorrhea
• Vasomotor symptoms associated with climacteric disturbance
• Vasomotor symptoms associated with ovarian deficiency symptoms

Off-label uses (4)

• Abnormal uterine bleeding unrelated to menstrual cycle
• Amenorrhea
• Dysmenorrhea
• Polycystic ovaries

Contraindications (60)

• Angina pectoris
• Asthma
• Benign mammary dysplasia
• Body fluid retention
• Breast lump
• Carcinoma of female breast
• Cardiovascular event risk
• Cerebrovascular accident
• Chloasma
• Cholestasis of pregnancy
• Chorea
• Chronic heart failure
• Deep venous thrombosis
• Dementia
• Depressive disorder
• Diabetes mellitus
• Disease of liver
• Disorder of coronary artery
• Disorder of gallbladder
• Endometrial carcinoma
• Epilepsy
• Estrogen receptor positive tumor
• Family history of malignant neoplasm of breast
• Functional visual loss
• Heart valve disorder
• Hepatic porphyria
• Humoral hypercalcemia of malignancy
• Hypercholesterolemia
• Hyperglycemia
• Hyperlipidemia
• + 30 more

Mechanism & targets

• Established pharmacologic class: Progestin

Molecular targets (9)

Target	Gene	Action	Activity
Progesterone receptor	PGR	agonist	ED50 11.26
Estrogen receptor	Esr1|Esr2	unknown	Kd 9.20
Progesterone receptor	PGR	unknown	Ki 8.91
Sex hormone-binding globulin	SHBG	unknown	Kd 7.97
Androgen receptor	AR	unknown	IC50 7.12
Androgen receptor	Ar	unknown	IC50 6.92
Glucocorticoid receptor	NR3C1	unknown	Ki 6.71
Estrogen receptor	ESR1	unknown	Ki 6.64
Sodium-dependent serotonin transporter	SLC6A4	unknown	Ki 5.62

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1962-05-21	FDA	—	ORTHO MCNEIL PHARM

ATC classification

ATC code	Therapeutic hierarchy
G03AA05	GENITO URINARY SYSTEM AND SEX HORMONES › SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM › HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE › Progestogens and estrogens, fixed combinations
G03AB04	GENITO URINARY SYSTEM AND SEX HORMONES › SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM › HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE › Progestogens and estrogens, sequential preparations
G03AC01	GENITO URINARY SYSTEM AND SEX HORMONES › SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM › HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE › Progestogens
G03DC02	GENITO URINARY SYSTEM AND SEX HORMONES › SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM › PROGESTOGENS › Estren derivatives
G03FA01	GENITO URINARY SYSTEM AND SEX HORMONES › SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM › PROGESTOGENS AND ESTROGENS IN COMBINATION › Progestogens and estrogens, fixed combinations
G03FB05	GENITO URINARY SYSTEM AND SEX HORMONES › SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM › PROGESTOGENS AND ESTROGENS IN COMBINATION › Progestogens and estrogens, sequential preparations
H01CC53	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS › PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES › HYPOTHALAMIC HORMONES › Anti-gonadotropin-releasing hormones
H01CC54	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS › PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES › HYPOTHALAMIC HORMONES › Anti-gonadotropin-releasing hormones

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
Hepatic adenoma	248.1
Vaginal haemorrhage	144.3
Metaplasia	113.6
Heavy menstrual bleeding	88.6
Prostatic disorder	81.6
Intermenstrual bleeding	73.4
Endometriosis	62.9
Aplastic anaemia	59.1
Pregnancy on oral contraceptive	49.7
Pelvic pain	49.3
Superior sagittal sinus thrombosis	48.1
Complication of device insertion	45.6

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Norethisterone is on its molecule page.

• Molecular formula: C₂₀H₂₆O₂
• Molecular weight: 298.43 g/mol
• CAS number: 68-22-4
• InChIKey: VIKNJXKGJWUCNN-XGXHKTLJSA-N
• PubChem CID: 6230

C[C@]12CC[C@H]3[C@@H](CCC4=CC(=O)CC[C@H]34)[C@@H]1CC[C@@]2(O)C#C

Frequently asked questions

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

What is Norethisterone used for?

DrugCentral lists the following indications for Norethisterone: Acne vulgaris, Atrophic vaginitis, Atrophic vulva, Contraception, Controlled ovarian stimulation, Dysfunctional uterine bleeding, Endometriosis and Female hypogonadism syndrome and others.

How does Norethisterone work?

Its molecular targets in DrugCentral include PGR (agonist), Esr1|Esr2, PGR and SHBG.

When was Norethisterone first approved?

Norethisterone was first approved by the FDA in 1962.

What drug class does Norethisterone belong to?

Norethisterone is in the Progestin class.

What is the chemical formula of Norethisterone?

Norethisterone has the molecular formula C20H26O2 and a molecular weight of 298.43 g/mol.

Sources

• DrugCentral drug card 1962 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1162 — compound record and bioactivity
• PubChem CID 6230 — chemical identifiers
• DrugBank DB00717 — drug record
• FDA UNII T18F433X4S — substance identity
• DailyMed: FDA labels for Norethisterone — current prescribing information (label search)
• UniProt P06401 (PGR) — target protein
• UniProt P04278 (SHBG) — target protein
• UniProt P10275 (AR) — target protein
• UniProt P04150 (NR3C1) — target protein
• UniProt P03372 (ESR1) — target protein
• UniProt P31645 (SLC6A4) — 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.