Toremifene citrate | 89778-27-8, Toremifene citrate Formula

Description

White-to-Off-White Solid

Toremifene citrate is a stilbenoid. It has a role as an anticoronaviral agent.|Toremifene Citrate is the citrate salt of a nonsteroidal triphenylethylene antiestrogen. Chemically related to tamoxifen, toremifene is a selective estrogen receptor modulator (SERM). This agent binds competitively to estrogen receptors, thereby interfering with estrogen activity. Toremifene also has intrinsic estrogenic properties, which is manifested depending on the tissue or species. (NCI04)|A first generation selective estrogen receptor modulator (SERM). Like TAMOXIFEN, it is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on mammary and uterine tissue.

Toremifene citrate Basic Attributes

Molecular Weight：

598.08

Exact Mass：

597.213

EC Number：

1308068-626-2

UNII：

2498Y783QT

NSC Number：

759190|613680

DSSTox ID：

DTXSID2021367

NCI Thesaurus Code：

C1756

ATC Code：

L02BA02

HScode：

2942000000

Characteristics

PSA：

145

XLogP3：

4.96650

Appearance：

white to off-white

Density：

1,045g/cm

Melting Point：

160-162 °C

Boiling Point：

146-148C

Flash Point：

277.4ºC

Refractive Index：

1.416-1.418

Water Solubility：

DMSO: >10mg/mL

Storage Conditions：

-20°C Freezer

Collision Cross Section：

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

Safety Information

Transport codes：

UN 3077 9 / PGIII

wgk germany：

3

hazard class code：

36/37/38-50/53-41-22

safety instructions：

26-37/39-61-60-39

RTECS Number：

KH2156700

Marks：

Xi,N,Xn

Precautionary statement(s)：

P264, P270, P273, P280, P301+P312, P305+P351+P338, P310, P330, P391, P501

Hazard Statements：

H302

GHS Classification：

|Danger|H302 (97.56%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P273, P280, P301+P312, P305+P351+P338, P310, P330, P391, and P501|Aggregated GHS information provided by 41 companies from 4 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Drug Indication：

First line hormone treatment of hormone-dependent metastatic breast cancer in postmenopausal patients., Fareston is not recommended for patients with estrogen receptor negative tumours.,|Drug: Toremifene

MeSH：

A structurally diverse group of compounds distinguished from ESTROGENS by their ability to bind and activate ESTROGEN RECEPTORS but act as either an agonist or antagonist depending on the tissue type and hormonal milieu. They are classified as either first generation because they demonstrate estrogen agonist properties in the ENDOMETRIUM or second generation based on their patterns of tissue specificity. (Horm Res 1997;48:155-63) (See all compounds classified as Selective Estrogen Receptor Modulators.)|Antineoplastic agents that are used to treat hormone-sensitive tumors. Hormone-sensitive tumors may be hormone-dependent, hormone-responsive, or both. A hormone-dependent tumor regresses on removal of the hormonal stimulus, by surgery or pharmacological block. Hormone-responsive tumors may regress when pharmacologic amounts of hormones are administered regardless of whether previous signs of hormone sensitivity were observed. The major hormone-responsive cancers include carcinomas of the breast, prostate, and endometrium; lymphomas; and certain leukemias. (From AMA Drug Evaluations Annual 1994, p2079) (See all compounds classified as Antineoplastic Agents, Hormonal.)|Agents that inhibit BONE RESORPTION and/or favor BONE MINERALIZATION and BONE REGENERATION. They are used to heal BONE FRACTURES and to treat METABOLIC BONE DISEASES such as OSTEOPOROSIS. (See all compounds classified as Bone Density Conservation Agents.)

MeSH Entry Terms：

Citrate, Toremifene

Toremifene citrate Use and Manufacturing

Uses

An antiestrogen and antineoplastic. Nonsteroidal antiestrogen structurally similar to Tamoxifen.

Use Classification：

Human drugs -> Fareston -> EMA Drug Category|Endocrine therapy -> Human pharmacotherapeutic group|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:598.1
Hydrogen Bond Donor Count:4
Hydrogen Bond Acceptor Count:9
Rotatable Bond Count:14
Exact Mass:597.2129448
Monoisotopic Mass:597.2129448
Topological Polar Surface Area:145
Heavy Atom Count:42
Complexity:710
Defined Bond Stereocenter Count:1
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Toremifene citrate is a nonsteroidal triphenylethylene derivative that binds to estrogen receptors to produce estrogen-like or anti-estrogen effects. It mainly exhibits anti-estrogen effects in humans and rats, and estrogen-like effects in mice. Toremifene administration in postmenopausal breast cancer patients caused a moderate decrease in serum total cholesterol and low-density lipoprotein (LDL). Its anti-breast cancer effect is mainly anti-estrogen, and there may be other anti-cancer mechanisms (changing tumor gene expression, secreting growth factors, inducing cell apoptosis, and affecting cell kinetic cycle).

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

Toremifene citrate
Ingredients	The main ingredient of this product is toremifene citrate.
Indication	No specific interaction studies have been conducted. Drugs that reduce renal excretion of calcium, such as thiazide diuretics, can increase hypercalcemia. Enzyme inducers such as phenytoin, phenobarbital, and carbamazepine can accelerate the excretion of toremifene, causing a decrease in steady-state serum concentrations. In this case, the daily dose may need to be doubled. It has been determined that anti-estrogen drugs and warfarin anticoagulants have a synergistic effect and cause a serious increase in bleeding time. Therefore, co-administration with such drugs should be avoided. Theoretically, the main metabolic pathway of toremifene is the CYP3A enzyme system. Drugs that have an inhibitory effect on this enzyme system, such as ketoconazole and similar antifungal drugs, erythromycin, and triacetyloleandromycin, can inhibit the metabolism of toremifene. Therefore, the simultaneous use of such drugs should be carefully considered.

Toremifene citrate

Ingredients

The main ingredient of this product is toremifene citrate.

Indication

No specific interaction studies have been conducted. Drugs that reduce renal excretion of calcium, such as thiazide diuretics, can increase hypercalcemia. Enzyme inducers such as phenytoin, phenobarbital, and carbamazepine can accelerate the excretion of toremifene, causing a decrease in steady-state serum concentrations. In this case, the daily dose may need to be doubled. It has been determined that anti-estrogen drugs and warfarin anticoagulants have a synergistic effect and cause a serious increase in bleeding time. Therefore, co-administration with such drugs should be avoided. Theoretically, the main metabolic pathway of toremifene is the CYP3A enzyme system. Drugs that have an inhibitory effect on this enzyme system, such as ketoconazole and similar antifungal drugs, erythromycin, and triacetyloleandromycin, can inhibit the metabolism of toremifene. Therefore, the simultaneous use of such drugs should be carefully considered.

Toremifene citrate
Indication	No specific interaction studies have been conducted. Drugs that reduce renal excretion of calcium, such as thiazide diuretics, can increase hypercalcemia. Enzyme inducers such as phenytoin, phenobarbital, and carbamazepine can accelerate the excretion of toremifene, causing a decrease in steady-state serum concentrations. In this case, the daily dose may need to be doubled. It has been determined that anti-estrogen drugs and warfarin anticoagulants have a synergistic effect and cause a serious increase in bleeding time. Therefore, co-administration with such drugs should be avoided. Theoretically, the main metabolic pathway of toremifene is the CYP3A enzyme system. Drugs that have an inhibitory effect on this enzyme system, such as ketoconazole and similar antifungal drugs, erythromycin, and triacetyloleandromycin, can inhibit the metabolism of toremifene. Therefore, the simultaneous use of such drugs should be carefully considered.
Manufacturer	Fuan Pharmaceutical Group Ningbo Team Pharmaceutical Co., Ltd.

Toremifene citrate

Indication

No specific interaction studies have been conducted. Drugs that reduce renal excretion of calcium, such as thiazide diuretics, can increase hypercalcemia. Enzyme inducers such as phenytoin, phenobarbital, and carbamazepine can accelerate the excretion of toremifene, causing a decrease in steady-state serum concentrations. In this case, the daily dose may need to be doubled. It has been determined that anti-estrogen drugs and warfarin anticoagulants have a synergistic effect and cause a serious increase in bleeding time. Therefore, co-administration with such drugs should be avoided. Theoretically, the main metabolic pathway of toremifene is the CYP3A enzyme system. Drugs that have an inhibitory effect on this enzyme system, such as ketoconazole and similar antifungal drugs, erythromycin, and triacetyloleandromycin, can inhibit the metabolism of toremifene. Therefore, the simultaneous use of such drugs should be carefully considered.

Manufacturer

Fuan Pharmaceutical Group Ningbo Team Pharmaceutical Co., Ltd.

Toremifene Citrate Tablets
Ingredients	Chemical name: Toremifene citrate Chemical structure: Molecular formula: C26H28CINO·C6H8O7 Molecular weight: 598.09
Indication	1. No specific interaction studies have been conducted. 2. Drugs that reduce renal excretion of calcium, such as thiazide diuretics, can increase hypercalcemia. 3. Enzyme inducers, such as phenytoin, phenobarbital, and carbamazepine, can accelerate the excretion of toremifene, causing a decrease in steady-state serum concentrations. In this case, the daily dose may need to be doubled. 4. It has been confirmed that anti-estrogen drugs and warfarin anticoagulants have a synergistic effect, causing a serious increase in bleeding time. Therefore, simultaneous use with such drugs should be avoided. 5. Theoretically, the main metabolic pathway of toremifene is the CYP3A enzyme system. Drugs that have an inhibitory effect on this enzyme system, such as ketoconazole and similar antifungal drugs, erythromycin, and triacetyloleandromycin, can inhibit the metabolism of toremifene. Therefore, simultaneous use with such drugs should be considered carefully.
Specifications	60 mg/tablet

See More Related Drugs

Registered Holders

MSN LABORATORIES PRIVATE LTD

United States
Active
TAI HENG INDUSTRY CO LTD

United States
Active
Fermion Oy

Finland
Active

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