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Halcinonide

Halcinonide structure

CAS No:
3093-35-4
Formula:
C24H32ClFO5
Chemical Name:
Halcinonide
Synonyms:
Pregn-4-ene-3,20-dione,21-chloro-9-fluoro-11-hydroxy-16,17-[(1-methylethylidene)bis(oxy)]-,(11β,16α)-;Pregn-4-ene-3,20-dione,21-chloro-9-fluoro-11β,16α,17-trihydroxy-,cyclic 16,17-acetal with acetone;2H-Naphth[2′,1′:4,5]indeno[1,2-d][1,3]dioxole,pregn-4-ene-3,20-dione deriv.;(11β,16α)-21-Chloro-9-fluoro-11-hydroxy-16,17-[(1-methylethylidene)bis(oxy)]pregn-4-ene-3,20-dione;Halcinonide;SQ 18566;Halog;Halciderm;Alcinonide;Adcortin;Halcimat;2205903-20-2
Categories:
Active Pharmaceutical Ingredients > Hormones and the Endocrine System

Description

Halcinonide (SQ-18566) is a high potency corticosteroid used topically in the treatment of certain skin conditions.

Halcinonide is an organic molecular entity. It has a role as a SMO receptor agonist.|Halcinonide is a corticosteroid indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses, and is distributed as a cream and ointment. Halcinonide is marketed under the brand name Halog® by Ranbaxy Laboratories Inc. Research suggests that clobetasol propionate demonstrates superior pharmacologic efficacy in the treatment of psoriasis when compared to halcinonide.|Halcinonide is a Corticosteroid. The mechanism of action of halcinonide is as a Corticosteroid Hormone Receptor Agonist.|Halcinonide is a topical, synthetic glucocorticoid with anti-inflammatory and anti-allergic properties. Halcinonide exerts its effect by interacting with specific intracellular receptors, and the ligand-receptor complex subsequently modulates gene expressions via the typical glucocorticoid signalling pathway. This results in the synthesis of certain anti-inflammatory proteins as well as in synthesis inhibition of certain inflammatory mediators. Consequently, an overall reduction in chronic inflammation and autoimmune reactions are accomplished. (NCI05)|A glucocorticoid used topically in the treatment of DERMATITIS; ECZEMA; or PSORIASIS. It may cause skin irritation.

Halcinonide Basic Attributes

Molecular Weight：

454.95900

Exact Mass：

454.96

EC Number：

221-439-6

UNII：

SI86V6QNEG

DSSTox ID：

DTXSID6045375

NCI Thesaurus Code：

C47552

ATC Code：

D - Dermatologicals

HScode：

2937220000

Characteristics

PSA：

72.83000

XLogP3：

3.88930

Density：

1.31 g/cm3

Melting Point：

264 °C (decomp)

Boiling Point：

564.3ºC at 760 mmHg

Flash Point：

295.1ºC

Refractive Index：

1.566

Storage Conditions：

Keep tightly closed. Store in a cool dry place.

Toxicity：

LD50 i.p. in mice: 150 mg/kg (Millonig, Yiakas)

Collision Cross Section：

200.9 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

hazard class code：

R63

safety instructions：

S36

RTECS Number：

TU5010200

Marks：

Stability/Shelf Life：

Stable at normal temperatures and pressures.

Precautionary statement(s)：

P280

Hazard Statements：

H361

GHS Classification：

|Warning|H361 (100%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]|P201, P202, P281, P308+P313, P405, and P501|Aggregated GHS information provided by 40 companies from 3 notifications to the ECHA C&L Inventory.

Toxicity

Toxicity Summary：

Systemic absorption of topical corticosteroids has produced reversible hypothalamicpituitary-adrenal (HPA) axis suppression, manifestations of Cushing’s syndrome, hyperglycemia, and glucosuria in some patients. Conditions which augment systemic absorption include the application of the more potent steroids, use over large surface areas, prolonged use, and the addition of occlusive dressings.

Drug Information

Drug Indication：

Indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.|FDA Label

MeSH：

Substances that reduce or suppress INFLAMMATION. (See all compounds classified as Anti-Inflammatory Agents.)

Mechanism of Action：

The precise mechanism of action of topical corticosteroids is unclear. However they possess anti-inflammatory, antipruritic, and vasoconstrictive actions. New research indicates that halcinonide activates MBP (myelin basic protein) expression via smoothened receptor activation. This finding suggests that halcinonide could be used in the treatment of multiple sclerosis therapy as an alternative to Dexamethasone or Methylprednisolone.

MeSH Entry Terms：

Alcinonide

Halcinonide Use and Manufacturing

Uses

A topical steroid. Used to treat inflammation caused by a number of conditions such as allergic reactions, eczema, and psoriasis.

Use Classification：

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients|Pharmaceuticals

Computed Properties

Molecular Weight:455.0
XLogP3:3.6
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:2
Exact Mass:454.1922300
Monoisotopic Mass:454.1922300
Topological Polar Surface Area:72.8
Heavy Atom Count:31
Complexity:887
Defined Atom Stereocenter Count:8
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Drug Function and Efficacy

This product is a highly effective fluorinated and chlorinated corticosteroid with anti-inflammatory, anti-pruritic and vasoconstrictive effects. Its anti-inflammatory and antipruritic mechanism is to increase the responsiveness of β receptors to catecholamine, increase CAMP production by activating adenylate cyclase, and inhibit phosphoethylesterase to reduce CAMP destruction, resulting in an increase in cAMP concentration in cells and inhibiting the release of histamine. This product has a similar effect as dexamethasone in inhibiting the proliferation of granulomas in rats and mice.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Halcinonide Cream
Ingredients	The main ingredients of this product and their chemical names are: Halcinonide (clofosinolone, halcinonide), 16α, 17-[(1-methylethylidene)bis(oxy)]-11β-hydroxy-21-chloro-9-fluoropregnane-4-ene-3,20-dione.
Indication	If you are using other medicines, you should consult your physician or pharmacist before using this product.
Specifications	10g:10mg
Manufacturer	Jiangsu Xinfu Pharmaceutical Co., Ltd.

Halcinonide solution
Ingredients	The main ingredients of this product and their chemical names are: Halcinonide (clofosinolone, halcinonide), 16α, 17-[(1-methylethylidene)bis(oxy)]-11β-hydroxy-21-chloro-9-fluoropregnane-4-ene-3,20-dione.
Indication	If you are using other medicines, you should consult your physician or pharmacist before using this product.
Specifications	0.1%
Manufacturer	Chongqing KERUI Pharmaceutical (GROUP) Co., Ltd.

Halcinonide Cream
Ingredients	The main ingredients of this product and their chemical names are: Halcinonide (clofosinolone, halcinonide), 16α, 17-[(1-methylethylidene)bis(oxy)]-11β-hydroxy-21-chloro-9-fluoropregnane-4-ene-3,20-dione.
Indication	If you are using other medicines, you should consult your physician or pharmacist before using this product.
Specifications	10g:10mg
Manufacturer	Teyi Pharmaceutical Group Co., Ltd.

See More Related Drugs

Registered Holders

FARMABIOS S.P.A.

Italy
Active
Jinyao Pharmaceutical Co., Ltd.

China
Active
Hunan Yuxin Pharmaceutical Co., Ltd.

China
Active

See More Registered Holders

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