Nolvadex: profile and news






Phase II Trial Explores Faslodex® After Aromatase Inhibitor  07 Mar 2006
Historically, the most common hormonal treatment for estrogen receptor-positive breast cancer was an antiestrogen called Nolvadex® (tamoxifen). ... - Cancer Consultants (press release),

Aromasin® Improves Breast Cancer Outcomes Without Compromising ...  Feb 28, 2006
Breast cancer patients who switched to Aromasin® (exemestane) after 2-3 years of Nolvadex® (tamoxifen) reported a similar quality of life to patients who ... - Cancer Consultants (press release),

BIG Results and Expanded Treatment Options  Feb 21, 2006
According to results from the Breast International Group (BIG) trial of Femara® (letrozole) versus Nolvadex® (tamoxifen), use of Femara for adjuvant ... - Cancer Consultants (press release),

Generalists Equal Specialists in Follow-Up Care for Early Breast ...  Feb 20, 2006
...for follow-up care, including schedules for physical exams, mammograms, diagnostic tests if needed, plus guidelines for patients taking Nolvadex (tamoxifen). ... - MedPage Today,

Is it safe to take Femara for breast cancer if I also have ...  Feb 9, 2006
...the Femara will be only marginally effective, you and your doctor may want to consider other medications for your breast cancer, such as tamoxifen (Nolvadex). ... - MayoClinic.com

Lessons on breast cancer: Risk, detection, treatment  Feb 10, 2006
If the patient has an ER-positive tumor, she may respond well to tamoxifen (Nolvadex), a drug that works by blocking the receptor site. ... - Charlotte Observer,

Phosphagenics initiates anti-cancer compound animal trials  Jan 25, 2006
...buoyed on by this encouraging preliminary data, which also claimed a significant advantage over the anti-breast cancer drug Nolvadex (tamoxifen citrate). ... - BiopharmaReporter.com,

Survival benefit for Arimidex in early breast cancer compared with ...  Jan 10, 2006
Three key international trials ( ABCSG - Austrian Breast & Colorectal Cancer Study Group 8 , ARNO - Arimidex-Nolvadex 95, and ITA – Italian Tamoxifen ... - Xagena.it,

Removal of Axillary Nodes Causes Significant Morbidity in Older ...  Jan 24, 2006
...lymph node dissection. Women in both study groups received five years of Nolvadex® (tamoxifen) as adjuvant therapy. The initial ... - Cancer Consultants (press release),

'My mother was sat beside me and I remember thinking 'If she's ...  Jan 7, 2006
This therapy, manufactured originally by ICI under the trade name Nolvadex before its mechanism was fully understood, blocked oestrogen production by adhering ... - The Observer,

Researchers Update Nolvadex® Prevention Trial  Nov 29, 2005
...affiliated with the National Surgical Adjuvant Breast and Bowel Project P-1 Study have reported a 7 year follow up confirming that Nolvadex (tamoxifen) lowers ... - Cancer Consultants (press release),

Deaths from Coronary Artery Disease Reduced with Long-Term ...  Nov 8, 2005
Swedish researchers have reported that 5 years of Nolvadex versus 2 years of Nolvadex reduces the incidence of coronary artery deaths by 33% as well as ... - Cancer Consultants (press release),

Adjuvant Nolvadex® Confirmed Ineffective for Receptor Negative ...  Nov 9, 2005
Researchers from Germany have confirmed previous studies showing that adjuvant Nolvadex (tamoxifen) does not prevent breast cancer recurrences in women with ... - Cancer Consultants (press release),

Faslodex® Provides Clinical Benefit for Women with Breast Cancer ...  Dec 1, 2005
Historically, the most common hormonal treatment for ER-positive breast cancer was an anti-estrogen called Nolvadex® (tamoxifen). ... - Cancer Consultants (press release),

Study shows tamoxifen can prevent cancer for years  Nov 15, 2005
Researchers found that women who took tamoxifen, sold as a generic and by AstraZeneca Plc under the brand Nolvadex, for up to five years were about 43 percent ... - Malaysia Star,

Study Finds Tamoxifen Reduces Long-Term Risk of Breast Cancer  Nov 16, 2005
The pre- and post-menopausal women who took tamoxifen (also marketed by AstraZeneca as a generic called Nolvadex) for five years or more were approximately 43 ... - Newsinferno.com,

Study shows tamoxifen can prevent cancer for years  Nov 16, 2005
...a placebo. Tamoxifen is sold in the United States as a generic drug as well as under the brand name Nolvadex by AstraZeneca. Out ... - The Advocate,

Canadian Regulators Warn Against Use of Femara as Fertility Drug  Nov 30, 2005
Extended adjuvant treatment of early breast cancer in postmenopausal women who have received five years of adjuvant therapy with Nolvadex (tamoxifen). ... - CNN

Adjuvant Tamoxifen Does Not Prevent Recurrences in Hormone ...  Nov 9, 2005
According to results recently published in the Journal of Clinical Oncology, use of the anti-estrogen agent tamoxifen (Nolvadex®) does not reduce recurrences ... - Cancer Consultants (press release),

Final Results from the NSABP Breast Cancer Prevention Trial ...  Nov 15, 2005
...into surrounding, healthy tissues) incidence among participants at increased risk for the disease who took tamoxifen (Nolvadex ® , AstraZeneca Pharmaceuticals ... - National Institutes of Health (press release)

Updated Results Confirm Tamoxifen Risks and Benefits  Nov 21, 2005
Breast and Bowel Project (NSABP) Breast Cancer Prevention Trial (P-1) began in 1992, with the goal of determining whether tamoxifen (Nolvadex®) could reduce ... - Cancer Consultants (press release),

AstraZeneca Provides Additional Support to Hurricane Victims  Nov 17, 2005
...calcium), EMLA Cream (lidocaine 2.5% and prilocaine 2.5%), FASLODEX® (fulvestrant), NEXIUM® (esomeprazole magnesium), NOLVADEX® (tamoxifen citrate), PLENDIL ... - Yahoo! News (press release)

Final results from the NSABP breast cancer prevention trial ...  Nov 16, 2005
...and is growing into surrounding, healthy tissues) incidence among participants at increased risk for the disease who took tamoxifen (Nolvadex(r), AstraZeneca ... - Biotech Intelligence (press release),

AstraZeneca Provides Additional Support to Hurricane Victims  Nov 17, 2005
...rosuvastatin calcium), EMLA Cream (lidocaine 2.5% and prilocaine 2.5%), FASLODEX(R) (fulvestrant), NEXIUM(R) (esomeprazole magnesium), NOLVADEX(R) (tamoxifen ... - PR Newswire (press release),

Updated Results: Femara® Following Nolvadex® in Breast Cancer  Sep 15, 2005
Researchers affiliated with the MA.17 trial have reported that the administration of Femara (letrozole) following 5 years of Nolvadex (tamoxifen) improves ... - Cancer Consultants (press release),

Aromasin® Approved for Early Breast Cancer  Oct 10, 2005
...exemestane) for treatment in early, hormone-positive breast cancer in postmenopausal women following two to three years of treatment with Nolvadex® (tamoxifen ... - Cancer Consultants (press release),

ARIMIDEX(R) (anastrozole) Gains Full FDA Approval for Adjuvant ...  Sep 19, 2005
Important Information About Tamoxifen: NOLVADEX(R) (tamoxifen citrate) is approved for the adjuvant treatment of node-positive and node-negative early breast ... - PR Newswire (press release),

ARIMIDEX (anastrozole) Gains Full FDA Approval for Adjuvant ...  Sep 20, 2005
NOLVADEX(R) (tamoxifen citrate) is approved for the adjuvant treatment of node-positive and node-negative early breast cancer in postmenopausal women following ... - PharmaLive.com (press release),

Options Update: Putting Pessimistic Bets on AstraZeneca  Oct 4, 2005
Continuing down the list of AZN's treatments, I see Atacand (a hypertension and heart failure drug), Crestor (a cholesterol reducer), Nolvadex (for breast ... - Schaeffers Research,

Breast cancer, an aromatase inhibitor, Letrozole, improves ...  Sep 10, 2005
...drug Letrozole ( Femara ) confirms earlier reports that the drug reduced the recurrence of breast cancer in women previously treated with Tamoxifen ( Nolvadex ... - Xagena.it,

Arimidex® Granted Full Approval for Early Breast Cancer  Sep 20, 2005
...cancer cells. Tamoxifen (Nolvadex®) was historically the most commonly used agent for hormone-positive breast cancer. However, agents ... - Cancer Consultants (press release),

Think Before You Pink  Sep 30, 2005
It produces Nolvadex (tamoxifen), the most widely prescribed breast cancer drug, which in 1994 brought in $470 million, as reported by Monte Paulsen in Mother ... - Chronogram,

AstraZeneca Receive Highly Coveted Frost & Sullivan Award ...  Sep 20, 2005
...of its current anti-cancer therapies including 'ARIMIDEX' (anastrozole), 'CASODEX' (bicalutamide), 'FASLODEX' (fulvestrant), 'NOLVADEX' (tamoxifen), 'ZOLADEX ... - PR Newswire (press release),

Results of Breast Cancer Study Confirm Benefit  Sep 8, 2005
...on the drug letrozole (Femara) confirms earlier studies that show the drug reduces breast cancer recurrence in women previously treated with tamoxifen (Nolvadex ... - Ivanhoe

Updated Results: Femara® Following Tamoxifen in Breast Cancer  08 Sep 2005
...longer follow-up from the clinical trial referred to as MA.17 continues to support the use of Femara® following 5 years of Nolvadex® (tamoxifen) in ... - Cancer Consultants (press release),

Endocrine Status Called Key to Breast Cancer Therapy  08 Sep 2005
The panel said that while there is evidence that chemotherapy and Nolvadex (tamoxifen) should not be given at the same time, no such evidence exists for the ... - MedPage Today,

New International Treatment Guidelines Verify Crucial Role of ' ...  Sep 7, 2005
...of its current anti-cancer therapies including 'ARIMIDEX' (anastrozole), 'CASODEX' (bicalutamide), 'FASLODEX' (fulvestrant), 'NOLVADEX' (tamoxifen), 'ZOLADEX ... - news aktuell (Pressemitteilung),

Adjuvant Chemotherapy has Improved Survival of Women with Poor ...  Aug 17, 2005
...of 568 patients who received chemotherapy with anthracycline-based chemotherapy between the years of 1974 and 1998, with or without Nolvadex® (tamoxifen). ... - Cancer Consultants (press release),

AstraZeneca Pledges More Than $1 Million in Contributions and ...  Sep 1, 2005
...calcium), EMLA Cream (lidocaine 2.5% and prilocaine 2.5%), FASLODEX® (fulvestrant), NEXIUM® (esomeprazole magnesium), NOLVADEX® (tamoxifen citrate), PLENDIL ... - Yahoo! News (press release)

AstraZeneca Pledges More Than $1 Million in Contributions and ...  Sep 1, 2005
...rosuvastatin calcium), EMLA Cream (lidocaine 2.5% and prilocaine 2.5%), FASLODEX(R) (fulvestrant), NEXIUM(R) (esomeprazole magnesium), NOLVADEX(R) (tamoxifen ... - PR Newswire (press release),

Breast cancer, switch to Anastrozole after two years of Tamoxifen ...  Aug 14, 2005
...published in The Lancet, demonstrated that switching treatment to the drug Anastrozole ( Arimidex ) after two years of Tamoxifen ( Nolvadex ) can improve event ... - Xagena.it,

Benefit With Aromatase Inhibitors in the Adjuvant Setting for ...  Aug 25, 2005
The Arimidex or Nolvadex (ARNO) and the small ITA (Italian Tamoxifen Arimidex) trials similarly sequenced anastrozole after tamoxifen and also found that ... - Medscape (subscription)

Cancer Prevention Studies Are Growing  Aug 4, 2005
The goal of STAR, which recruited more than 20,000 women, is to determine which drug – tamoxifen (Nolvadex®) or raloxifene (Evista®) – is more effective ... - CancerWise

FDA Considers Expanding Femara  Jul 11, 2005
...or in women with "estrogen receptor positive" cancer, Femara is not associated with the same side effects as tamoxifen, marketed as Nolvadex, which include hot ... - WebProNews

Approval sought for Femara in early post-surgery use  Jul 12, 2005
...which showed that Femara reduced the risk of the cancer recurring by 19 percent more than tamoxifen, which is made by AstraZeneca under the brand name Nolvadex ... - News-Medical.net

Novartis files Femara for early post-surgery use  Jul 11, 2005
...and used tamoxifen, Novartis said. Tamoxifen is made by AstraZeneca under the brand name Nolvadex. While aromatase inhibitors have ... - Reuters


Other information


Indication
for the treatment of breast cancer

Pharmacology
Tamoxifen belongs to a class of drugs called selective estrogen receptor modulators (SERMs), which have both estrogenic and antiestrogenic effects. Tamoxifen has the same nucleus as diethylstilbestrol but possesses an additional side chain (trans isomer) which accounts for its antiestrogenic activity. Tamoxifen, chemically related to clomiphene., is used to in the therapy of metastatic breast cancer.

Mechanism Of Action
Tamoxifen binds to estrogen receptors (ER), inducing a conformational change in the receptor. This results in a blockage or change in the expression of estrogen dependent genes. The prolonged binding of tamoxifen to the nuclear chromatin of these results in reduced DNA polymerase activity, impaired thymidine utilization, blockade of estradiol uptake, and decreased estrogen response. It is likely that tamoxifen interacts with other coactivators or corepressors in the tissue and binds with different estrogen receptors, ER-alpha or ER-beta, producing both estrogenic and antiestrogenic effects.

Drug Category
Antineoplastic Agents; ATC:L02BA01

Brand Names/Synonyms
,Citrate; Apo-Tamox; CCRIS 3275; CTX; Citofen; Crisafeno; Diemon; Gen-Tamoxifen; HSDB 6782; Istubol; Kessar; Noltam; Nolvadex; Nolvadex-D; Nourytam; Novo-Tamoxifen; Oncomox; Pms-Tamoxifen; Retaxim; TRANS FORM OF TAMOXIFEN; Tamizam; Tamofen; Tamone; Tamoxasta; Tamoxen; Tamoxifen; Tamoxifen Citrate; Tamoxifen Drug Standard Solution; Tamoxifen and Its Salts; Tamoxifene [Inn-French]; Tamoxifeno [Inn-Spanish]; Tamoxifenum [Inn-Latin]; Trans-Tamoxifen; Valodex; Zemide

Dosage Forms
TABLET

Absorption
Not Available

Interactions
-->Interactions for Tamoxifen:

When NOLVADEX is used in combination with coumarin-type anticoagulants, a significant increase in anticoagulant effect may occur. Where such coadministration exists, careful monitoring of the patientís prothrombin time is recommended.

In the NSABP P-1 trial, women who required coumarin-type anticoagulants for any reason were ineligible for participation in the trial.

There is an increased risk of thromboembolic events occurring when cytotoxic agents are used in combination with NOLVADEX.

Tamoxifen reduced letrozole plasma concentrations by 37%. The effect of tamoxifen on metabolism and excretion of other antineoplastic drugs, such as cyclophosphamide and other drugs that require mixed function oxidases for activation, is not known. Tamoxifen and N-desmethyl tamoxifen plasma concentrations have been shown to be reduced when coadministered with rifampin or aminoglutethimide. Induction of CYP3A4-mediated metabolism is considered to be the mechanism by which these reductions occur; other CYP3A4 inducing agents have not been studied to confirm this effect.

One patient receiving NOLVADEX with concomitant phenobarbital exhibited a steady state serum level of tamoxifen lower than that observed for other patients (ie, 26 ng/mL vs. mean value of 122 ng/mL). However, the clinical significance of this finding is not known. Rifampin induced the metabolism of tamoxifen and significantly reduced the plasma concentrations of tamoxifen in 10 patients. Aminoglutethimide reduces tamoxifen and N desmethyl tamoxifen plasma concentrations. Medroxyprogesterone reduces plasma concentrations of N-desmethyl, but not tamoxifen.

Concomitant bromocriptine therapy has been shown to elevate serum tamoxifen and N-desmethyl tamoxifen.

Drug/Laboratory Testing Interactions:

During postmarketing surveillance, T4 elevations were reported for a few postmenopausal patients which may be explained by increases in thyroid-binding globulin. These elevations were not accompanied by clinical hyperthyroidism.

Variations in the karyopyknotic index on vaginal smears and various degrees of estrogen effect on Pap smears have been infrequently seen in postmenopausal patients given NOLVADEX.

In the postmarketing experience with NOLVADEX, infrequent cases of hyperlipidemias have been reported. Periodic monitoring of plasma triglycerides and cholesterol may be indicated in patients with pre-existing hyperlipidemias .

 

 


Chemical IUPAC Name
[5-(2-amino-6-oxo-3,9-dihydropurin-9-yl)-3,4-dihydroxy-tetrahydrofuran-2-yl]methoxy-[(3,4-dihydroxy-6-methyl-5-oxo-tetrahydropyran-2-yl)oxy-hydroxy-phosphoryl]oxy-phosphinicacid

Chemical Formula
C16H23N5O15P2

Half Life
5-7 days

Drug Type
Approved Drug

# Accession No
APRD00123

CAS Registry Number
10540-29-1


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