Drug intelligence / Profile preview

anastrozole + risedronate

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

The combination of anastrozole and risedronate is used primarily in postmenopausal women with hormone receptor-positive breast cancer who are at risk of bone loss due to anastrozole treatment. This combination therapy addresses a significant side effect of aromatase inhibitor treatment while maintaining the cancer-fighting benefits. ## Drug Information Anastrozole is an aromatase inhibitor that works by reducing estrogen production, which is beneficial for treating hormone receptor-positive breast cancer in postmenopausal women[1][2]. However, this reduction in estrogen can lead to bone mineral density (BMD) loss and increased fracture risk[3][4]. Risedronate is a bisphosphonate that helps prevent bone loss by inhibiting osteoclast-mediated bone resorption. When combined with anastrozole, risedronate has been shown to significantly improve BMD at both the lumbar spine and hip in postmenopausal breast cancer patients[1][2]. ## Clinical Evidence Multiple clinical trials have demonstrated the efficacy of this combination: - A multicenter, phase III prospective open-label clinical trial showed that after 24 months, patients receiving anastrozole plus risedronate experienced a significant increase in BMD at the lumbar spine (+5.7%) and hip (+1.6%) compared to decreases in those receiving anastrozole alone (-1.5% and -3.9%, respectively)[1]. - In high-risk (osteoporotic) patients, the combination therapy resulted in significant BMD increases at the lumbar spine at both 12 and 24 months (6.3% and 6.6%, respectively)[1]. - Another study demonstrated that adding 35 mg oral risedronate weekly to anastrozole improved BMD both at lumbar spine (+6.8%) and femoral neck (+2.8%) after 24 months in osteopenic postmenopausal breast cancer women[2]. ## Safety Profile The combination therapy is generally well-tolerated. Common adverse events include: - Mild gastrointestinal symptoms (abdominal pain, indigestion, nausea, diarrhea, and constipation)[2] - Musculoskeletal symptoms (primarily in anastrozole-only patients)[2] - No cases of osteonecrosis of the jaw were observed in patients on risedronate treatment during the studies[2] Importantly, the combination of anastrozole and risedronate has been shown to have a neutral effect on lipid profiles, with no clinically significant changes in LDL-C, HDL-C, total cholesterol, or serum triglycerides after 12 months of treatment[3]. ## Recommendations Based on the clinical evidence, the combination of anastrozole plus oral risedronate is recommended for postmenopausal breast cancer patients receiving anastrozole who have pre-existing osteopenia or osteoporosis to prevent aromatase inhibitor-related bone loss[1][2]. Patients with normal BMD before starting treatment with anastrozole have a very low risk of developing osteoporosis and may not require the combination therapy[1]. All patients receiving this combination therapy should also receive daily supplements of calcium (1000 mg/day) and vitamin D (400 IU/day)[1].

02

Targets

FDPS (Farnesyl pyrophosphate synthase)CYP19A1 (Aromatase)

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