Exemestane: Package Insert and Label Information (Page 4 of 5)

14.2 Treatment of Advanced Breast Cancer

Exemestane 25 mg administered once daily was evaluated in a randomized double-blind, multicenter, multinational comparative study and in two multicenter single-arm studies of postmenopausal women with advanced breast cancer who had disease progression after treatment with tamoxifen for metastatic disease or as adjuvant therapy. Some patients also have received prior cytotoxic therapy, either as adjuvant treatment or for metastatic disease.

The primary purpose of the three studies was evaluation of objective response rate (complete response [CR] and partial response [PR]). Time to tumor progression and overall survival were also assessed in the comparative trial. Response rates were assessed based on World Health Organization (WHO) criteria, and in the comparative study, were submitted to an external review committee that was blinded to patient treatment. In the comparative study, 769 patients were randomized to receive exemestane tablets 25 mg once daily (N = 366) or megestrol acetate 40 mg four times daily (N = 403). Demographics and baseline characteristics are presented in Table 9.

Table 9. Demographics and Baseline Characteristics from the Comparative Study of Postmenopausal Women with Advanced Breast Cancer Whose Disease Had Progressed after Tamoxifen Therapy
ParameterExemestane(N = 366)Megestrol Acetate(N = 403)
Median Age (range)65 (35–89)65 (30–91)
ECOG Performance Status
0167 (46%)187 (46%)
1162 (44%)172 (43%)
234 (9%)42 (10%)
Receptor Status
ER and/or PgR +246 (67%)274 (68%)
ER and PgR unknown116 (32%)128 (32%)
Responders to prior tamoxifen68 (19%)85 (21%)
NE for response to prior tamoxifen46 (13%)41 (10%)
Site of Metastasis
Visceral ± other sites207 (57%)239 (59%)
Bone only61 (17%)73 (18%)
Soft tissue only54 (15%)51 (13%)
Bone & soft tissue43 (12%)38 (9%)
Measurable Disease287 (78%)314 (78%)
Prior Tamoxifen Therapy
Adjuvant or Neoadjuvant145 (40%)152 (38%)
Advanced Disease, Outcome
CR, PR, or SD ≥ 6 months179 (49%)210 (52%)
SD < 6 months, PD or NE42 (12%)41 (10%)
Prior Chemotherapy
For advanced disease ± adjuvant58 (16%)67 (17%)
Adjuvant only104 (28%)108 (27%)
No chemotherapy203 (56%)226 (56%)

The efficacy results from the comparative study are shown in Table 10. The objective response rates observed in the two treatment arms showed that exemestane was not different from megestrol acetate. Response rates for exemestane from the two single-arm trials were 23.4% and 28.1%.

Table 10. Efficacy Results from the Comparative Study of Postmenopausal Women with Advanced Breast Cancer Whose Disease Had Progressed after Tamoxifen Therapy
Response CharacteristicsExemestane(N=366)Megestrol Acetate(N=403)
Abbreviations: CR = complete response, PR = partial response, SD = stable disease (no change), TTP = time to tumor progression, C.I. = confidence interval, MA = megestrol acetate, AR = Exemestane
Objective Response Rate = CR + PR (%)15.012.4
Difference in Response Rate (AR-MA)2.6
95% C.I.7.5, -2.3
CR (%)2.21.2
PR (%)12.811.2
SD ≥ 24 Weeks (%)21.321.1
Median Duration of Response (weeks)76.171.0
Median TTP (weeks)20.316.6
Hazard Ratio (AR-MA)0.84

There were too few deaths occurring across treatment groups to draw conclusions on overall survival differences. The Kaplan-Meier curve for time to tumor progression in the comparative study is shown in Figure 2.

Figure 2. Time to Tumor Progression in the Comparative Study of Postmenopausal Women With Advanced Breast Cancer Whose Disease Had Progressed After Tamoxifen Therapy

Figure 2
(click image for full-size original)

16 HOW SUPPLIED/STORAGE AND HANDLING

Exemestane Tablets, USP are white or almost white round film-coated tablets, debossed with 111 on one side. Each tablet contains 25 mg of exemestane, USP.

Exemestane Tablets, USP are packaged in HDPE bottles with a child-resistant screw cap, supplied in packs as follows.

Bottle of 30 NDC 71921-190-33

Bottle of 90 NDC 71921-190-09

Store at 25°C (77ºF); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature].

17 PATIENT COUNSELING INFORMATION

Advise the patient to read the FDA approved patient labeling (Patient Information).

Bone Effects

Advise patients that exemestane lowers the level of estrogen in the body. This may lead to reduction in bone mineral density (BMD) over time. The lower the BMD, the greater the risk of osteoporosis and fracture [see Warnings and Precautions (5.1)].

Other Estrogen-Containing Agents

Advise patients that they should not take estrogen-containing agents while they are taking exemestane as these could interfere with its pharmacologic action [see Warnings and Precautions (5.3)].

Use in Premenopausal Women

Advise patients that exemestane is not for use for the treatment of breast cancer in premenopausal women [see Warnings and Precautions (5.5)].

Embryo-Fetal Toxicity

Advise pregnant women and females of reproductive potential that exposure during pregnancy or within 1 month prior to conception can result in fetal harm. Advise females to inform their healthcare provider of a known or suspected pregnancy [see Warnings and Precautions (5.6) and Use in Specific Populations (8.1)].

Advise females of reproductive potential to use effective contraception while taking exemestane and for 1 month after the last dose [see Use in Specific Populations (8.3)].

Lactation

Advise women not to breastfeed during treatment with exemestane and for 1 month after the last dose [see Use in Specific Populations (8.2)].

Manufactured by:

Qilu Pharmaceutical Co., Ltd.
Jinan, 250104, China

Manufactured for:

Florida Pharmaceutical Products, LLCBoca Raton, 33487, FL, USA

Revised: 1/2022

Code number: 34040094511B

Patient InformationExemestane (EX-e-MES-tane) Tablets, USP
This Patient Information has been approved by the U.S. Food and Drug Administration Revised: 1/2022

What is exemestane?

Exemestane is used in women who are past menopause for the treatment of:

  • Early breast cancer (cancer that has not spread outside the breast) in women who:
    • have cancer that needs the female hormone estrogen to grow, and
    • have had other treatments for breast cancer, and
    • have taken tamoxifen for 2 to 3 years, and
    • are switching to exemestane to complete 5 years in a row of hormonal therapy.
  • Advanced breast cancer (cancer that has spread) after treatment with tamoxifen, and it did not work or is no longer working.

It is not known if exemestane is safe and effective in children.

Do not take exemestane if you are allergic to exemestane or any of the ingredients in exemestane. See the end of this leaflet for a complete list of ingredients in exemestane.

Before you take exemestane, tell your doctor about all your medical conditions, including if you:

  • are still having menstrual periods (are not past menopause). Exemestane is only for women who are past menopause.
  • have weak or brittle bones (osteoporosis)
  • are pregnant or plan to become pregnant. Taking exemestane during pregnancy or within 1 month of becoming pregnant can harm your unborn baby.
    • Females who are able to become pregnant should have a pregnancy test within 7 days before starting treatment with exemestane.
    • Females who are able to become pregnant should use effective birth control (contraceptive) during treatment with exemestane and for 1 month after your last dose of exemestane. Tell your doctor right away if you become pregnant or think you may be pregnant.
  • are breastfeeding or plan to breastfeed. It is not known if exemestane passes into your breast milk. Do not breast-feed during treatment with exemestane and for 1 month after your last dose of exemestane.
  • Have liver or kidney problems.

Tell your doctor about all the medicines you take, including prescription and over-the-counter medicines, vitamins and herbal supplements. Especially tell your doctor if you take medicines that contain estrogen, including other hormone replacement therapy or birth control pills or patches. Exemestane should not be taken with medicines that contain estrogen as they could affect how well exemestane works.

How should I take exemestane?

  • Take exemestane exactly as your doctor tells you.
  • Take exemestane 1 time each day after a meal.
  • If you take too much exemestane, call your doctor right away or go to nearest hospital emergency room.

What are the possible side effects of exemestane?

Exemestane may cause serious side effects, including:

  • Bone loss. Exemestane decreases the amount of estrogen in your body which may reduce your bone mineral density (BMD) over time. This may increase your risk for bone fractures or weak and brittle bones (osteoporosis). Your doctor may check your bones during treatment with exemestane if you have osteoporosis or at risk for osteoporosis.

The most common side effects of exemestane in women with early breast cancer include:

  • hot flashes
  • headache
  • feeling tired
  • trouble sleeping
  • joint pain
  • increased sweating

The most common side effects of exemestane in women with advanced breast cancer include:

  • hot flashes
  • increased sweating
  • nausea
  • increased appetite
  • feeling tired

Your doctor will do blood tests to check your vitamin D level before starting treatment with exemestane.

Exemestane may cause decreased fertility in males and females. Talk to your doctor if you have concerns about fertility.

These are not all the possible side effects of exemestane. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

How should I store exemestane?

  • Store exemestane at room temperature 68°F to 77°F (20°C to 25°C).
  • Keep exemestane and all medicines out of the reach of children.

General information about the safe and effective use of exemestane.

Medicines are sometimes prescribed for purposes other than those listed in a Patient Information leaflet. Do not use exemestane for a condition for which it was not prescribed. Do not give exemestane to other people, even if they have the same symptoms you have. It may harm them. You can ask your pharmacist or doctor for information about exemestane that is written for health professionals.

What is in exemestane tablets?

Active ingredient: exemestane, USP

Inactive ingredients: mannitol, polysorbate 80, hypromellose, colloidal silicon dioxide, microcrystalline cellulose, sodium starch glycolate, magnesium stearate, talc, polyethylene glycol 3350, titanium dioxide, and polyvinyl alcohol.

Manufactured by:

Qilu Pharmaceutical Co., Ltd.Jinan, 250104, China

Manufactured for:Florida Pharmaceutical Products, LLCBoca Raton, 33487, FL, USA

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