Hormone Receptors and Endocrine Therapy in Breast Cancer
Sherry X. Yang, Janet E. Dancey in Handbook of Therapeutic Biomarkers in Cancer, 2021
Based on the existing evidence, tamoxifen 20 mg daily is recommended as adjuvant endocrine therapy for premenopausal women with HR+ invasive breast cancer by major practice guidelines. The ASCO recommends tamoxifen for at least 5 years for premenopausal women and those who remain premenopausal can continue tamoxifen for another 5 years for a total of 10 years. If a patient becomes menopausal after the first 5 years of treatment, she can continue the drug for an additional 5 years or switch to an AI for 5 more years in a total of 10 years. The National Comprehensive Cancer Network (NCCN) recommends that tamoxifen can be used alone if tumors are small (<0.5 cm) or have micro-invasion with minimal lymph node involvement (<2 mm in axillary node metastasis). If tumors are >0.5 cm but with minimal lymph node involvement, the endocrine therapy is indicated regardless of whether chemotherapy is recommended. For patients with node-positive disease, tamoxifen is given after chemotherapy and radiation therapy [47]. Based on the OncoType Dx assay, patients with the recurrence scores of 0–25 can receive tamoxifen or other hormonal agents alone (see details in Chapter 13). Tamoxifen is well tolerated in general. The major known side effects include hot flashes, thromboembolic events and endometrial cancer (Table 5.1). Tamoxifen is teratogenic and premenopausal patients taking tamoxifen should avoid pregnancy. Tamoxifen reduces bone density in premenopausal women but promotes bone density in postmenopausal women [48]. Bisphosphonates are used to prevent bone loss.
Management of bone pain
Nigel Sykes, Michael I Bennett, Chun-Su Yuan in Clinical Pain Management, 2008
Bisphosphonates are a class of drug originally developed for use in metabolic bone disease, such as osteoporosis and Paget’s disease. The first generation drugs such as etidronate have subsequently been replaced with the development of more potent drugs. The most commonly used currently are clodronate, pamidronate, and zolendronate, which have an increasing role in the management of metastatic bone disease. Their mode of action is through inhibiting the function of osteoclasts. Since the initial response in the process of a bone metastasis being established is osteoclast activation, they have been investigated as a potential means of inhibiting the development of bone metastasis in patients who are at high risk. There are now phase III randomized placebo-controlled trial data supporting this effect in myeloma52 [II] and breast cancer.53, 54[II] Although the magnitude of effect is relatively modest, bisphosphonates are standard adjuvant treatment in myeloma and breast cancer patients at high risk of bone metastases.
Role of bisphosphonates and denosumab
Peter V. Giannoudis, Thomas A. Einhorn in Surgical and Medical Treatment of Osteoporosis, 2020
Bisphosphonates are a class of agents that have been widely used as the first-line treatment of osteoporosis and a number of other conditions involving excessive bone resorption, including skeletal complications of malignancy, osteogenesis imperfecta, and Paget disease. Etidronate, the first bisphosphonate approved in the United States, was used in 1968 to treat a young patient with myositis ossificans progressive. Etidronate was considered to also have several other potential benefits, including the capacity to prevent heterotopic ossification after total hip replacement and spinal cord injury. Then, in the 1970s, with more bisphosphonates available, these medications were employed to treat a number of conditions such as Paget disease and hypercalcemia of malignancy. In the 1990s, after bone densitometry use widened, bisphosphonates became standard treatment for patients diagnosed with osteoporosis. For more than 40 years, bisphosphonates have been used worldwide for the treatment of osteoporosis (6).
Risedronate-loaded aerogel scaffolds for bone regeneration
Published in Drug Delivery, 2023
Nahla El-Wakil, Rabab Kamel, Azza A. Mahmoud, Alain Dufresne, Ragab E. Abouzeid, Mahmoud T. Abo El-Fadl, Amr Maged
In this study, the fabricated 3D aerogel scaffolds were used as a carrier for risedronate. Bisphosphonates are therapeutic agents used for the treatment of bone disorders. The regular turnover of bone is maintained by a balance between the actions of osteoblasts (cells that build bone) and osteoclasts (bone destroying cells). Bisphosphonates decrease bone loss by inhibiting the action of osteoclasts (Weinstein et al., 2009). Loading the scaffolds with a drug inhibiting bone resorption like bisphosphonates can optimize the treatment of bone defects. Therefore, cellulose-based 3D aerogel scaffolds, loaded with risedronate, were prepared by chemical cross-linking (with amorphous cellulose) or physical cross-linking (with chitosan), and they were evaluated for their physicochemical and cell regenerative properties.
Improvement of bone microarchitecture in methylprednisolone induced rat model of osteoporosis by using thiolated chitosan-based risedronate mucoadhesive film
Published in Drug Development and Industrial Pharmacy, 2018
Dhrubojyoti Mukherjee, Bharath Srinivasan, J. Anbu, Mohammad Azamthulla, Venkatesh Teja Banala, S. G. Ramachandra
The treatment of osteoporosis has been dominated by antiresorptive agents like zoledronate, risedronate, alendronate, etc., which are bisphosphonate derivatives. These agents prevent further bone loss [1]. Osteoporosis is a serious condition in post-menopausal women, old age group male, and children who are malnourished. By 2050, the worldwide number of hip fracture cases due to osteoporosis are expected to rise by about 310% in men and 240% in women [2]. Osteoporotic fractures have a great impact on public health because they are frequently associated with enhanced mortality and economic cost [3]. Bisphosphonates are the synthetic analogs of the inorganic pyrophosphate, a naturally occurring polyphosphate present in serum and urine, which can bind with the newly formed crystals of hydroxyapatite and thereby prevent calcification of bone [4]. Bisphosphonates are generally used for the treatment of osteoporosis, bone metastasis, and Paget’s disease. After administration, bisphosphonates are rapidly cleared from the circulation and localize to the bone surface at the sites of active bone remodeling in the areas undergoing osteoclasts (OCT) induced resorption [5].
Hypercalcemia and acute kidney injury induced by eldecalcitol in patients with osteoporosis: a case series of 32 patients at a single facility
Published in Renal Failure, 2019
Seishi Aihara, Shunsuke Yamada, Hideaki Oka, Taro Kamimura, Toshiaki Nakano, Kazuhiko Tsuruya, Atsumi Harada
Osteoporosis is a common disease characterized by decreased bone strength, low bone mass, and skeletal fragility, which increase the risk of bone fracture [1]. In Japan, older subjects make up 26.7% of the total population, and osteoporosis in the older generation is a major public health problem [2]. To date, there have been several classes of drugs prescribed for patients with osteoporosis. Among them, bisphosphonates, which inhibit bone resorption and maintain a positive bone-remodeling balance [3], have been used as a first-line treatment for osteoporosis because they have been shown to greatly reduce the risk for bone fracture. However, bisphosphonates have the potential to cause serious side effects such as osteonecrosis of the jaw, atypical femoral fracture, and esophageal ulcer, and are not always the best treatment option. Hence, some of the patients with osteoporosis are still being treated with vitamin D receptor activators (VDRAs).
Related Knowledge Centers
- Bone Density
- Osteoporosis
- Phosphonate
- Bone
- Bone REModeling
- Homeostasis
- Osteoblast
- Osteoclast
- Apoptosis
- Paget'S Disease of Bone