WALTHAM, MA, USA I July 15, 2015 I Radius Health, Inc. (“Radius” or “we”) (RDUS), a science-driven biopharmaceutical company developing new therapeutics for patients with advanced osteoporosis as well as other serious endocrine-mediated diseases including hormone responsive metastatic breast cancer, today announced that early but promising preclinical data show that its investigational drug RAD1901, in combination with CDK4/6 inhibitors, such as Pfizer’s palbociclib and mTOR inhibitors, such as Novartis’ everolimus, was effective in shrinking tumors.
In breast cancer models using patient derived xenografts with either wild type or mutant ESR1, treatment with RAD 1901 resulted in marked tumor growth inhibition, but the combination of RAD1901 with either agent, palbociclib or everolimus, showed anti-tumor activity that was significantly greater than either agent alone. RAD1901 is being evaluated at high doses as a Selective Estrogen Receptor Degrader (SERD) for potential use in metastatic breast cancer.
In addition to this preclinical study, Radius has also recently completed a pharmacokinetic/ pharmacodynamic study in healthy volunteers. In total, 52 subjects were treated with doses between 200 mg and 1000mg for up to 7 days. Preliminary data suggested that all doses were generally well tolerated. A subset of subjects received baseline and FES-PET after 7 days to evaluate ER signal attenuation, and we expect to report the final results of this study in the third quarter of this year.
Separately, an abstract titled “RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models” of the preclinical characterization, anti-tumor activity and therapeutic potential of investigational drug RAD1901 in breast cancer has been published in the online journal Anti-Cancer Drugs, and can be found at http://journals.lww.com/anticancerdrugs/Abstract/publishahead/RAD1901.
“These data provide Radius with important insights to evaluate multiple options including combination therapies as we seek to accelerate the next phases of our clinical development program for RAD1901 in metastatic breast cancer,” said Robert E. Ward, President and CEO of Radius Health.
Radius is currently screening and enrolling patients in a Phase 1 multicenter, open-label, two-part, dose-escalation study of the investigational drug RAD1901 in postmenopausal women with advanced estrogen receptor positive and HER2-negative breast cancer. The study is designed to determine the recommended Phase 2 dose of RAD1901, and includes a preliminary evaluation of the potential anti-tumor effects. Following the determination of an optimal dose, Radius plans to initiate trials in a larger expansion cohort to evaluate the potential role of the investigational drug RAD1901 in combination with currently available therapies.
About the Investigational Drug RAD1901
Radius is developing the investigational drug RAD1901 as a potential treatment for estrogen positive (ER+) cancers, like breast, ovarian or endometrial cancer. Currently, Radius is focusing its clinical research activities in breast cancer. The National Cancer Institute estimates that approximately 70% of breast cancers are ER+ and may grow in response to exposure to estrogen. Endocrine therapy is intended to block the estrogen signal or reduce the production of estrogen. More information about breast cancer and endocrine therapy may be found on the National Cancer Institute website http://www.cancer.gov/cancertopics/factsheet/Therapy/hormone-therapy-breast.
RAD1901 is an investigational, non-steroidal small molecule that is designed to selectively bind and degrade the ER. RAD1901 has demonstrated potent anti-tumor activity in xenograft models of ER+ breast cancer in preclinical testing and complete suppression of the FES-PET signal after six days of dosing in a maximum tolerated dose clinical study. In preclinical models thus far, RAD1901 has shown good tissue selectivity, does not appear to stimulate the uterine endometrium, and appears to protect against bone loss in an ovariectomy-induced osteopenia rat model. In addition, we believe that RAD1901 also has the ability to cross the blood-brain barrier. In vitro, treatment of human breast cancer cell lines with the investigational drug RAD1901 resulted in degradation of the ER and inhibition of both basal and estradiol-stimulated proliferation.
Radius has begun a Phase 1 multicenter, open-label, two-part, dose-escalation study of the investigational drug RAD1901 in postmenopausal women with advanced estrogen receptor positive and HER2-negative breast cancer. The study is designed to determine the recommended Phase 2 dose of RAD1901, and includes a preliminary evaluation of the potential anti-tumor effects. The incidence of dose limiting toxicities will be assessed during the first 28 days. Tumor response will be evaluated in patients with measurable or evaluable disease, using RECISTv1.1 guidelines every 8 weeks until the date of first documented progression or date of death from any cause, whichever comes first, assessed up to 12 months of treatment. Plasma concentrations of RAD1901 will be assessed every 28 days for up to 12 months of treatment. The details of the Phase 1 study of RAD1901 are posted on www.clinicaltrials.gov.
Radius is also developing RAD1901 at lower doses as a Selective Estrogen Receptor Modulator (SERM) , for the potential treatment of vasomotor symptoms. Historically, hormone replacement therapy (“HRT”) with estrogen or progesterone was considered the most efficacious approach to relieving menopausal symptoms such as hot flashes. However, because of the concerns about the potential long-term risks and contraindications associated with HRT, Radius believes a significant need exists for new therapeutic treatment options to treat vasomotor symptoms. In a Phase 2 proof of concept study, RAD1901 at lower doses demonstrated a reduction in the frequency and severity of moderate and severe hot flashes. Radius intends to commence a Phase 2b trial in vasomotor symptoms in the second half of 2015.
About Radius Health
Radius is a science-driven biopharmaceutical company developing new therapeutics for patients with advanced osteoporosis as well as other serious endocrine-mediated diseases including hormone responsive cancers. Radius’ lead development candidate is the investigational drug abaloparatide for subcutaneous injection, currently in Phase 3 development for potential use in the reduction of fracture risk in postmenopausal women with severe osteoporosis. The Radius clinical portfolio also includes an investigational abaloparatide transdermal patch for potential use in osteoporosis and the investigational drug RAD1901 for potential use in hormone driven, or hormone resistant, metastatic breast cancer, including breast cancer brain metastases. www.radiuspharm.com
SOURCE: Radius Health
Post Views: 123
WALTHAM, MA, USA I July 15, 2015 I Radius Health, Inc. (“Radius” or “we”) (RDUS), a science-driven biopharmaceutical company developing new therapeutics for patients with advanced osteoporosis as well as other serious endocrine-mediated diseases including hormone responsive metastatic breast cancer, today announced that early but promising preclinical data show that its investigational drug RAD1901, in combination with CDK4/6 inhibitors, such as Pfizer’s palbociclib and mTOR inhibitors, such as Novartis’ everolimus, was effective in shrinking tumors.
In breast cancer models using patient derived xenografts with either wild type or mutant ESR1, treatment with RAD 1901 resulted in marked tumor growth inhibition, but the combination of RAD1901 with either agent, palbociclib or everolimus, showed anti-tumor activity that was significantly greater than either agent alone. RAD1901 is being evaluated at high doses as a Selective Estrogen Receptor Degrader (SERD) for potential use in metastatic breast cancer.
In addition to this preclinical study, Radius has also recently completed a pharmacokinetic/ pharmacodynamic study in healthy volunteers. In total, 52 subjects were treated with doses between 200 mg and 1000mg for up to 7 days. Preliminary data suggested that all doses were generally well tolerated. A subset of subjects received baseline and FES-PET after 7 days to evaluate ER signal attenuation, and we expect to report the final results of this study in the third quarter of this year.
Separately, an abstract titled “RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models” of the preclinical characterization, anti-tumor activity and therapeutic potential of investigational drug RAD1901 in breast cancer has been published in the online journal Anti-Cancer Drugs, and can be found at http://journals.lww.com/anticancerdrugs/Abstract/publishahead/RAD1901.
“These data provide Radius with important insights to evaluate multiple options including combination therapies as we seek to accelerate the next phases of our clinical development program for RAD1901 in metastatic breast cancer,” said Robert E. Ward, President and CEO of Radius Health.
Radius is currently screening and enrolling patients in a Phase 1 multicenter, open-label, two-part, dose-escalation study of the investigational drug RAD1901 in postmenopausal women with advanced estrogen receptor positive and HER2-negative breast cancer. The study is designed to determine the recommended Phase 2 dose of RAD1901, and includes a preliminary evaluation of the potential anti-tumor effects. Following the determination of an optimal dose, Radius plans to initiate trials in a larger expansion cohort to evaluate the potential role of the investigational drug RAD1901 in combination with currently available therapies.
About the Investigational Drug RAD1901
Radius is developing the investigational drug RAD1901 as a potential treatment for estrogen positive (ER+) cancers, like breast, ovarian or endometrial cancer. Currently, Radius is focusing its clinical research activities in breast cancer. The National Cancer Institute estimates that approximately 70% of breast cancers are ER+ and may grow in response to exposure to estrogen. Endocrine therapy is intended to block the estrogen signal or reduce the production of estrogen. More information about breast cancer and endocrine therapy may be found on the National Cancer Institute website http://www.cancer.gov/cancertopics/factsheet/Therapy/hormone-therapy-breast.
RAD1901 is an investigational, non-steroidal small molecule that is designed to selectively bind and degrade the ER. RAD1901 has demonstrated potent anti-tumor activity in xenograft models of ER+ breast cancer in preclinical testing and complete suppression of the FES-PET signal after six days of dosing in a maximum tolerated dose clinical study. In preclinical models thus far, RAD1901 has shown good tissue selectivity, does not appear to stimulate the uterine endometrium, and appears to protect against bone loss in an ovariectomy-induced osteopenia rat model. In addition, we believe that RAD1901 also has the ability to cross the blood-brain barrier. In vitro, treatment of human breast cancer cell lines with the investigational drug RAD1901 resulted in degradation of the ER and inhibition of both basal and estradiol-stimulated proliferation.
Radius has begun a Phase 1 multicenter, open-label, two-part, dose-escalation study of the investigational drug RAD1901 in postmenopausal women with advanced estrogen receptor positive and HER2-negative breast cancer. The study is designed to determine the recommended Phase 2 dose of RAD1901, and includes a preliminary evaluation of the potential anti-tumor effects. The incidence of dose limiting toxicities will be assessed during the first 28 days. Tumor response will be evaluated in patients with measurable or evaluable disease, using RECISTv1.1 guidelines every 8 weeks until the date of first documented progression or date of death from any cause, whichever comes first, assessed up to 12 months of treatment. Plasma concentrations of RAD1901 will be assessed every 28 days for up to 12 months of treatment. The details of the Phase 1 study of RAD1901 are posted on www.clinicaltrials.gov.
Radius is also developing RAD1901 at lower doses as a Selective Estrogen Receptor Modulator (SERM) , for the potential treatment of vasomotor symptoms. Historically, hormone replacement therapy (“HRT”) with estrogen or progesterone was considered the most efficacious approach to relieving menopausal symptoms such as hot flashes. However, because of the concerns about the potential long-term risks and contraindications associated with HRT, Radius believes a significant need exists for new therapeutic treatment options to treat vasomotor symptoms. In a Phase 2 proof of concept study, RAD1901 at lower doses demonstrated a reduction in the frequency and severity of moderate and severe hot flashes. Radius intends to commence a Phase 2b trial in vasomotor symptoms in the second half of 2015.
About Radius Health
Radius is a science-driven biopharmaceutical company developing new therapeutics for patients with advanced osteoporosis as well as other serious endocrine-mediated diseases including hormone responsive cancers. Radius’ lead development candidate is the investigational drug abaloparatide for subcutaneous injection, currently in Phase 3 development for potential use in the reduction of fracture risk in postmenopausal women with severe osteoporosis. The Radius clinical portfolio also includes an investigational abaloparatide transdermal patch for potential use in osteoporosis and the investigational drug RAD1901 for potential use in hormone driven, or hormone resistant, metastatic breast cancer, including breast cancer brain metastases. www.radiuspharm.com
SOURCE: Radius Health
Post Views: 123
