AstraZeneca’s Faslodex met primary endpoint in first-line treatment of advanced breast cancer

On May 27, 2016 AstraZeneca reported positive results from the Phase III FALCON trial comparing Faslodex 500mg (fulvestrant) to Arimidex 1mg (anastrozole) for the treatment of locally-advanced or metastatic breast cancer, in post-menopausal women who have not had prior hormonal treatment for hormone-receptor-positive (HR+) breast cancer (Press release, AstraZeneca, MAY 27, 2016, View Source [SID:1234512823]).

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Faslodex 500mg demonstrated superiority compared with Arimidex 1mg in FALCON, and met its primary endpoint of extended progression-free survival. The trial showed an adverse event profile generally consistent with current knowledge of the safety profile of the medicines.

Sean Bohen, Executive Vice President, Global Medicines Development and Chief Medical Officer at AstraZeneca, said: "The FALCON results bring us closer to offering more and earlier treatment options to postmenopausal women with HR+ locally-advanced or metastatic breast cancer; the potential to delay disease progression is important for these patients as there is currently no cure. Faslodex has over 10 years of clinical evidence and we are committed to exploring its potential along with the rest of our outstanding oncology portfolio."

A full evaluation of the data is ongoing and the results are expected to be presented at a medical meeting in 2016.

Aromatase inhibitors (such as Arimidex) are the current standard of care in first-line treatment for postmenopausal women with advanced HR+ breast cancer1.

Faslodex 500mg is approved for the treatment of postmenopausal women with oestrogen-receptor (ER)-positive locally-advanced or metastatic breast cancer whose cancer has progressed following anti-oestrogen therapy2. Most recently, on 2 March 2016, the US Food and Drug Administration approved Faslodex 500mg, in combination with palbociclib, for the treatment of women with hormone-receptor-positive, human-epidermal-growth-factor-receptor 2-negative (HER2-) advanced or metastatic breast cancer (MBC), whose cancer has progressed after endocrine therapy3.

About FALCON

The FALCON (Fulvestrant and AnastrozoLe COmpared in hormonal therapy Naïve advanced breast cancer) trial is a Phase III, randomised, double-blind, multicentre trial. The trial compared the anti-tumour effects and tolerability profile of a 500mg dose of Faslodex plus placebo with a 1mg dose of Arimidex plus placebo, in postmenopausal women with hormone-receptor-positive, locally-advanced or metastatic breast cancer who have not been treated previously with any hormonal therapy.

About Advanced breast cancer (ABC)

ABC is the most advanced stage of breast cancer (stage IV), and occurs when cancer cells have spread beyond the initial tumour site to other parts of the body outside of the breast. Since there is no cure for ABC, the goal of current treatment is to delay disease progression4.

About Faslodex 500mg (fulvestrant)

Faslodex 500mg is indicated for the treatment of postmenopausal women with ER+, locally-advanced or metastatic breast cancer for disease relapse on or after adjuvant anti-oestrogen therapy, or disease progression on therapy with an anti-oestrogen.2

In the US, Faslodex 500mg is also approved, in combination with palbociclib, for the treatment of US women with HR+, human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer (MBC), whose cancer has progressed after endocrine therapy. Faslodex 500mg represents a hormonal therapy approach that helps to slow tumour growth by blocking and degrading the oestrogen receptor – a key driver of disease progression5.

Amgen Receives Positive CHMP Opinion To Extend Indication Of Kyprolis® (Carfilzomib) For The Treatment Of Relapsed Multiple Myeloma

On May 27, 2016 Amgen (NASDAQ:AMGN) reported that the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency has adopted a positive opinion to extend the current indication for Kyprolis (carfilzomib) to include treatment in combination with dexamethasone alone for adult patients with multiple myeloma who have received at least one prior therapy (Press release, Amgen, MAY 27, 2016, View Source [SID:1234512821]).

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"In the first ever comparative Phase 3 head-to-head study of two proteasome inhibitors in relapsed multiple myeloma, Kyprolis in combination with dexamethasone nearly doubled progression-free survival compared to a current standard of care regimen," said Sean E. Harper, M.D., executive vice president of Research and Development at Amgen. "We are pleased that the CHMP has recognized these robust data with a positive opinion, and we look forward to ensuring approval of this extended indication of Kyprolis."

The CHMP positive opinion is based on data from the Phase 3 head-to-head ENDEAVOR study in which patients with multiple myeloma treated with Kyprolis plus dexamethasone achieved superior progression-free survival (PFS) of 18.7 months compared to 9.4 months in those receiving Velcade (bortezomib) plus dexamethasone, (HR=0.53; 95 percent CI: 0.44,0.65 p<0.0001). The most common adverse reactions that occurred in greater than 20 percent of patients in the Kyprolis arm were anemia, fatigue, diarrhea, thrombocytopenia, nausea, pyrexia, dyspnea, respiratory tract infection, cough and peripheral edema.

The CHMP positive opinion will now be reviewed by the European Commission (EC) and if granted, the marketing authorization will be extended to include Kyprolis in combination with dexamethasone in the 28 member countries of the European Union, as well as Iceland, Lichtenstein and Norway. The extended indication adopted by the CHMP is: Kyprolis in combination with either lenalidomide and dexamethasone or dexamethasone alone is indicated for the treatment of adult patients with multiple myeloma who have received at least one prior therapy.

The EC previously granted marketing authorization for Kyprolis in combination with lenalidomide and dexamethasone for the treatment of adult patients with multiple myeloma who have received at least one prior therapy based on results of the ASPIRE study in November 2015. Today’s CHMP positive opinion follows the U.S. Food and Drug Administration’s approval of a supplemental New Drug Application based on the ENDEAVOR results in January 2016.

About Multiple Myeloma

Multiple myeloma is characterized by a recurring pattern of remission and relapse.1 It is a rare and very aggressive orphan disease that accounts for approximately one percent of all cancers worldwide.2-4 In Europe, approximately 39,000 patients are diagnosed with multiple myeloma each year and 24,000 patient deaths are reported on an annual basis.5

About ENDEAVOR

The randomized ENDEAVOR (RandomizEd, OpeN Label, Phase 3 Study of Carfilzomib Plus DExamethAsone Vs Bortezomib Plus DexamethasOne in Patients With Relapsed Multiple Myeloma) trial of 929 patients evaluated Kyprolis in combination with low-dose dexamethasone, versus bortezomib with low-dose dexamethasone in patients whose multiple myeloma has relapsed after at least one, but not more than three prior therapeutic regimens. The primary endpoint of the trial was PFS, defined as the time from treatment initiation to disease progression or death. In a clinical trial, measuring the PFS is one way to demonstrate how well a treatment works.6

This study was conducted at 235 sites worldwide. For information about this trial, please visit www.clinicaltrials.gov under trial identification number NCT01568866.

About Kyprolis (carfilzomib)

Proteasomes play an important role in cell function and growth by breaking down proteins that are damaged or no longer needed.7 Kyprolis has been shown to block proteasomes, leading to an excessive build-up of proteins within cells.7 In some cells, Kyprolis can cause cell death, especially in myeloma cells because they are more likely to contain a higher amount of abnormal proteins.7,8

Kyprolis is approved in the U.S. for the following:

In combination with dexamethasone or with lenalidomide plus dexamethasone for the treatment of patients with relapsed or refractory multiple myeloma who have received one to three lines of therapy.
As a single agent for the treatment of patients with relapsed or refractory multiple myeloma who have received one or more lines of therapy.
Kyprolis is also approved in Argentina, Israel, Kuwait, Mexico, Thailand, Colombia, Korea, Canada, Switzerland, Russia and the European Union. Additional regulatory applications for Kyprolis are underway and have been submitted to health authorities worldwide.

For more information, please visit www.kyprolis.com.

Important EU Product Safety Information

This medicinal product is subject to additional monitoring. This will allow quick identification of new safety information. Healthcare professionals are asked to report any suspected adverse reactions.

Kyprolis treatment should be supervised by a physician experienced in the use of anti-cancer therapy. The most serious side effects that may occur during Kyprolis treatment include: Cardiac toxicity, pulmonary toxicities, pulmonary hypertension, dyspnea, hypertension including hypertensive crises, acute renal failure, tumor lysis syndrome, infusion reactions, thrombocytopenia, hepatic toxicity, posterior reversible encephalopathy syndrome (PRES) and thrombotic thrombocytopenic purpura/hemolytic uremic syndrome (TTP/HUS). The most common side effects are anemia, fatigue, diarrhea, thrombocytopenia, nausea, pyrexia, dyspnea, respiratory tract infection, cough and peripheral edema.

Please refer to the Summary of Product Characteristics for full European prescribing information.

Important U.S. Product Safety Information

Cardiac Toxicities

New onset or worsening of pre-existing cardiac failure (e.g., congestive heart failure, pulmonary edema, decreased ejection fraction), restrictive cardiomyopathy, myocardial ischemia, and myocardial infarction including fatalities have occurred following administration of KYPROLIS. Some events occurred in patients with normal baseline ventricular function. Death due to cardiac arrest has occurred within one day of KYPROLIS administration.
Monitor patients for clinical signs or symptoms of cardiac failure or cardiac ischemia. Evaluate promptly if cardiac toxicity is suspected. Withhold KYPROLIS for Grade 3 or 4 cardiac adverse events until recovery, and consider whether to restart KYPROLIS at 1 dose level reduction based on a benefit/risk assessment.
While adequate hydration is required prior to each dose in Cycle 1, monitor all patients for evidence of volume overload, especially patients at risk for cardiac failure. Adjust total fluid intake as clinically appropriate in patients with baseline cardiac failure or who are at risk for cardiac failure.
Patients ≥ 75 years, the risk of cardiac failure is increased. Patients with New York Heart Association Class III and IV heart failure, recent myocardial infarction, conduction abnormalities, angina, or arrhythmias may be at greater risk for cardiac complications and should have a comprehensive medical assessment (including blood pressure and fluid management) prior to starting treatment with KYPROLIS and remain under close follow-up.
Acute Renal Failure

Cases of acute renal failure and renal insufficiency adverse events (including renal failure) have occurred in patients receiving KYPROLIS. Acute renal failure was reported more frequently in patients with advanced relapsed and refractory multiple myeloma who received KYPROLIS monotherapy. Monitor renal function with regular measurement of the serum creatinine and/or estimated creatinine clearance. Reduce or withhold dose as appropriate.
Tumor Lysis Syndrome

Cases of Tumor Lysis Syndrome (TLS), including fatal outcomes, have occurred in patients receiving KYPROLIS. Patients with multiple myeloma and a high tumor burden should be considered at greater risk for TLS. Adequate hydration is required prior to each dose in Cycle 1, and in subsequent cycles as needed. Consider uric acid lowering drugs in patients at risk for TLS. Monitor for evidence of TLS during treatment and manage promptly. Withhold KYPROLIS until TLS is resolved.
Pulmonary Toxicity

Acute Respiratory Distress Syndrome (ARDS), acute respiratory failure, and acute diffuse infiltrative pulmonary disease such as pneumonitis and interstitial lung disease have occurred in patients receiving KYPROLIS. Some events have been fatal. In the event of drug‐induced pulmonary toxicity, discontinue KYPROLIS.
Pulmonary Hypertension

Pulmonary arterial hypertension (PAH) was reported in patients treated with KYPROLIS. Evaluate with cardiac imaging and/or other tests as indicated. Withhold KYPROLIS for PAH until resolved or returned to baseline and consider whether to restart KYPROLIS based on a benefit/risk assessment.
Dyspnea

Dyspnea was reported in patients treated with KYPROLIS. Evaluate dyspnea to exclude cardiopulmonary conditions including cardiac failure and pulmonary syndromes. Stop KYPROLIS for Grade 3 or 4 dyspnea until resolved or returned to baseline. Consider whether to restart KYPROLIS based on a benefit/risk assessment.
Hypertension

Hypertension, including hypertensive crisis and hypertensive emergency, has been observed with KYPROLIS. Some of these events have been fatal. Monitor blood pressure regularly in all patients. If hypertension cannot be adequately controlled, withhold KYPROLIS and evaluate. Consider whether to restart KYPROLIS based on a benefit/risk assessment.
Venous Thrombosis

Venous thromboembolic events (including deep venous thrombosis and pulmonary embolism) have been observed with KYPROLIS. Thromboprophylaxis is recommended for patients being treated with the combination of KYPROLIS with dexamethasone or with lenalidomide plus dexamethasone. The thromboprophylaxis regimen should be based on an assessment of the patient’s underlying risks.
Patients using oral contraceptives or a hormonal method of contraception associated with a risk of thrombosis should consider an alternative method of effective contraception during treatment with KYPROLIS in combination with dexamethasone or lenalidomide plus dexamethasone.
Infusion Reactions

Infusion reactions, including life‐threatening reactions, have occurred in patients receiving KYPROLIS. Symptoms include fever, chills, arthralgia, myalgia, facial flushing, facial edema, vomiting, weakness, shortness of breath, hypotension, syncope, chest tightness, or angina. These reactions can occur immediately following or up to 24 hours after administration of KYPROLIS. Premedicate with dexamethasone to reduce the incidence and severity of infusion reactions. Inform patients of the risk and of symptoms of an infusion reaction and to contact a physician immediately if they occur.
Thrombocytopenia

KYPROLIS causes thrombocytopenia with recovery to baseline platelet count usually by the start of the next cycle. Thrombocytopenia was reported in patients receiving KYPROLIS. Monitor platelet counts frequently during treatment with KYPROLIS. Reduce or withhold dose as appropriate.
Hepatic Toxicity and Hepatic Failure

Cases of hepatic failure, including fatal cases, have been reported during treatment with KYPROLIS. KYPROLIS can cause increased serum transaminases. Monitor liver enzymes regularly regardless of baseline values. Reduce or withhold dose as appropriate.
Thrombotic Microangiopathy

Cases of thrombotic microangiopathy, including thrombotic thrombocytopenic purpura/hemolytic uremic syndrome (TTP/HUS), including fatal outcome have occurred in patients receiving KYPROLIS. Monitor for signs and symptoms of TTP/HUS. Discontinue KYPROLIS if diagnosis is suspected. If the diagnosis of TTP/HUS is excluded, KYPROLIS may be restarted. The safety of reinitiating KYPROLIS therapy in patients previously experiencing TTP/HUS is not known.
Posterior Reversible Encephalopathy Syndrome (PRES)

Cases of PRES have occurred in patients receiving KYPROLIS. PRES was formerly known as Reversible Posterior Leukoencephalopathy Syndrome. Consider a neuro‐radiological imaging (MRI) for onset of visual or neurological symptoms. Discontinue KYPROLIS if PRES is suspected and evaluate. The safety of reinitiating KYPROLIS therapy in patients previously experiencing PRES is not known.
Embryo-fetal Toxicity

KYPROLIS can cause fetal harm when administered to a pregnant woman based on its mechanism of action and findings in animals.
Females of reproductive potential should be advised to avoid becoming pregnant while being treated with KYPROLIS. Males of reproductive potential should be advised to avoid fathering a child while being treated with KYPROLIS. If this drug is used during pregnancy, or if pregnancy occurs while taking this drug, the patient should be apprised of the potential hazard to the fetus.
ADVERSE REACTIONS

The most common adverse reactions occurring in at least 20% of patients treated with KYPROLIS in the combination therapy trials: anemia, neutropenia, diarrhea, dyspnea, fatigue, thrombocytopenia, pyrexia, insomnia, muscle spasm, cough, upper respiratory tract infection, hypokalemia.
The most common adverse reactions occurring in at least 20% of patients treated with KYPROLIS in monotherapy trials: anemia, fatigue, thrombocytopenia, nausea, pyrexia, dyspnea, diarrhea, headache, cough, edema peripheral.

Full prescribing information for the U.S. is available at www.kyprolis.com.

Caladrius Biosciences Licenses Cell Therapy Technology for Ovarian Cancer and Subleases Irvine Facility to AiVita Biomedical

On May 26, 2016 Caladrius Biosciences, Inc. (NASDAQ:CLBS) ("Caladrius" or the "Company"), a cell therapy company combining an industry-leading development and manufacturing services provider (PCT) with a select therapeutic development pipeline, reported that it has licensed to AiVita Biomedical, Inc. ("AiVita") the exclusive global rights to its tumor cell/dendritic cell technology for the treatment of ovarian cancer (Press release, Caladrius Biosciences, MAY 26, 2016, View Source [SID1234528899]). In return, Caladrius will receive certain development milestone payments as well as royalties on sales of any commercial product. This transaction supports the Company’s strategy to monetize non-core assets. Under the license agreement AiVita will assume responsibility for all costs to develop a product using the licensed intellectual property, including the maintenance costs of the associated intellectual property.

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The license contributes to AiVita’s intellectual property protection for its next generation immunotherapy targeting cancer stem cells. AiVita intends to begin a Phase II clinical trial to evaluate the efficacy of its novel appoach for ovarian cancer in 2016. To facilitate these clinical objectives, AiVita has also assumed a sublease of the Company’s former Irvine, California facility. This sublease obligation will cover for the remainder of the lease term all cash obligations of Caladrius with respect to the rent and overhead of the Irvine facility.

"Licensing this technology to AiVita is another step forward in streamlining our strategic focus and reducing our operating expenses while monetizing non-core assets through royalty and other milestone-driven transactions," said David J. Mazzo, Ph.D., Chief Executive Officer of Caladrius. "This agreement adds to the one signed in February 2016 whereby we licensed to AiVita exclusive global rights to our cell-derived dermatological technology for topical skin applications."

Kyprolis® (Carfilzomib) Demonstrates Economic Value In Relapsed Or Refractory Multiple Myeloma Manuscript Published In "Journal of Medical Economics"

On May 26, 2016 Amgen (NASDAQ:AMGN) reported that the Kyprolis Global Economic Model (K-GEM)1 has been published in the Journal of Medical Economics showing that in the United States (U.S.), Kyprolis (carfilzomib) in combination with lenalidomide and dexamethasone (KRd) is cost-effective compared to lenalidomide and dexamethasone (Rd) alone in patients with relapsed or refractory multiple myeloma (Press release, Amgen, MAY 26, 2016, View Source;p=RssLanding&cat=news&id=2172860 [SID:1234512822]). The K-GEM demonstrated an incremental cost-effectiveness ratio of $107,250 per Quality-Adjusted Life Year (QALY). Kyprolis provides substantial value when its cost per QALY is contrasted against willingness-to-pay estimates of $150,000-$300,000 per QALY, which are cited as reasonable benchmarks for cancer in the U.S.2-4

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"We recognize that there are different methods, assumptions and perspectives needed to assess the value of innovation," said Joshua Ofman, M.D., M.S.H.S., senior vice president of Global Value and Access at Amgen. "The K-GEM was developed with input from experts worldwide as one of the multiple perspectives needed to assess value. Robust analysis, relying on clinical trial data to assess cost-effectiveness analysis is one approach that can help inform payer and provider decision-making related to value and costs. Ultimately, individual patient treatment decisions for diseases like multiple myeloma should be made by doctors and their patients, based on sound clinical data and evidence-based practice guidelines."

"Each time a patient with multiple myeloma experiences a relapse, the ability to achieve and sustain a meaningful response to treatment declines, so we continue to seek better ways of treating patients with this complex disease.5 For the healthcare system, each relapse means the disease burden and cost of care increases," said Andrzej Jakubowiak, M.D., Ph.D., lead author of the manuscript. "The rigorous approach taken in the K-GEM demonstrates the economic value of the KRd regimen over standard of care, with clear evidence of compelling value for patients, payers and society."

The K-GEM incorporated data directly from a head-to-head Phase 3 trial (ASPIRE) in patients with relapsed or refractory multiple myeloma who had received one to three prior therapies. The ASPIRE trial showed that treatment with KRd resulted in a significant improvement (additional 8.6 months) in median progression-free survival (PFS) compared to Rd (26.3 months vs. 17.6 months, hazard ratio for progression or death = 0.69; 95 percent confidence interval [CI]: 0.57 to 0.83; p<0.0001).6 The most common adverse reactions leading to discontinuation in the KRd arm included pneumonia (1 percent), myocardial infarction (0.8 percent) and upper respiratory tract infection (0.8 percent). A critical assumption in economic models of cancer and also the K-GEM, where trial results have not matured sufficiently to fully characterize the extent of survival, is the extrapolation of overall survival. While a common evidence-based practice in health economics, it should not be considered a claim of extended survival.

About the Kyprolis Global Economic Model
The Kyprolis Global Economic Model (K-GEM) provides a robust framework for considering the value of Kyprolis in combination with lenalidomide and dexamethasone in patients with relapsed or refractory multiple myeloma. It was co-developed with experts worldwide over a number of years, and has been used as the basis for a number of statutory Health Technology Assessment analyses around the world. The K-GEM incorporated data directly from a comparative Phase 3 trial (ASPIRE) in patients with relapsed multiple myeloma who had received one to three prior therapies.

About ASPIRE
The international, randomized Phase 3 ASPIRE (CArfilzomib, Lenalidomide, and DexamethaSone versus Lenalidomide and Dexamethasone for the treatment of PatIents with Relapsed Multiple MyEloma) trial evaluated Kyprolis in combination with lenalidomide and dexamethasone (KRd), versus lenalidomide and dexamethasone (Rd) alone, in patients with relapsed multiple myeloma following treatment with one to three prior regimens.6 The primary endpoint of the trial was PFS, defined as the time from treatment initiation to disease progression or death.6 Secondary endpoints included overall survival (OS), overall response rate (ORR), duration of response (DOR), disease control rate, health-related quality of life (HR-QoL) and safety.6 Patients were randomized to receive Kyprolis (20 mg/m2 on days 1 and 2 of cycle one only, escalating to 27 mg/m2 on days 8, 9, 15 and 16 of cycle one and continuing on days 1, 2, 8, 9, 15 and 16 of subsequent cycles), in addition to a standard dosing schedule of lenalidomide (25 mg per day for 21 days on, 7 days off) and low-dose dexamethasone (40 mg per week in four-week cycles), versus lenalidomide and low-dose dexamethasone alone.6 The study randomized 792 patients at sites in North America, Europe and Israel.

About Multiple Myeloma
Multiple myeloma is an incurable blood cancer, characterized by a recurring pattern of remission and relapse.7 It is a disease that, in 2012, accounted for approximately one percent of all cancers globally.8,9 In the U.S., there were more than 95,000 people living with, or in remission from, multiple myeloma in 2013.10

About Amgen’s Commitment to Oncology
Amgen Oncology is committed to helping patients take on some of the toughest cancers, such as those that have been resistant to drugs, those that progress rapidly through the body and those where limited treatment options exist. Amgen’s supportive care treatments help patients combat certain side effects of strong chemotherapy, and our targeted medicines and immunotherapies focus on more than a dozen different malignancies, ranging from blood cancers to solid tumors. With decades of experience providing therapies for cancer patients, Amgen continues to grow its portfolio of innovative and biosimilar oncology medicines.

About Kyprolis (carfilzomib)
Proteasomes play an important role in cell function and growth by breaking down proteins that are damaged or no longer needed.11 Kyprolis has been shown to block proteasomes, leading to an excessive build-up of proteins within cells.11 In some cells, Kyprolis can cause cell death, especially in myeloma cells because they are more likely to contain a higher amount of abnormal proteins.11,12 The irreversibility of Kyprolis’ binding has also been shown to offer a more sustained inhibition of the targeted enzymes.12

Kyprolis is approved in the U.S. for the following:

In combination with dexamethasone or with lenalidomide plus dexamethasone for the treatment of patients with relapsed or refractory multiple myeloma who have received one to three lines of therapy.
As a single agent for the treatment of patients with relapsed or refractory multiple myeloma who have received one or more lines of therapy.
Kyprolis is also approved in Argentina, Israel, Kuwait, Mexico, Thailand, Colombia, Korea, Canada, Switzerland and Russia and the European Union. Additional regulatory applications for Kyprolis are underway and have been submitted to health authorities worldwide.

For more information, please visit www.kyprolis.com.

Important Safety Information Regarding Kyprolis (carfilzomib) for Injection

INDICATION(S)

KYPROLIS (carfilzomib) is indicated in combination with dexamethasone or with lenalidomide plus dexamethasone for the treatment of patients with relapsed or refractory multiple myeloma who have received one to three lines of therapy.
KYPROLIS (carfilzomib) is indicated as a single agent for the treatment of patients with relapsed or refractory multiple myeloma who have received one or more lines of therapy.
IMPORTANT SAFETY INFORMATION

Cardiac Toxicities

New onset or worsening of pre-existing cardiac failure (e.g., congestive heart failure, pulmonary edema, decreased ejection fraction), restrictive cardiomyopathy, myocardial ischemia, and myocardial infarction including fatalities have occurred following administration of KYPROLIS. Some events occurred in patients with normal baseline ventricular function. Death due to cardiac arrest has occurred within one day of KYPROLIS administration.
Monitor patients for clinical signs or symptoms of cardiac failure or cardiac ischemia. Evaluate promptly if cardiac toxicity is suspected. Withhold KYPROLIS for Grade 3 or 4 cardiac adverse events until recovery, and consider whether to restart KYPROLIS at 1 dose level reduction based on a benefit/risk assessment.
While adequate hydration is required prior to each dose in Cycle 1, monitor all patients for evidence of volume overload, especially patients at risk for cardiac failure. Adjust total fluid intake as clinically appropriate in patients with baseline cardiac failure or who are at risk for cardiac failure.
Patients > 75 years, the risk of cardiac failure is increased. Patients with New York Heart Association Class III and IV heart failure, recent myocardial infarction, conduction abnormalities, angina, or arrhythmias may be at greater risk for cardiac complications and should have a comprehensive medical assessment (including blood pressure and fluid management) prior to starting treatment with KYPROLIS and remain under close follow-up.
Acute Renal Failure

Cases of acute renal failure and renal insufficiency adverse events (including renal failure) have occurred in patients receiving KYPROLIS. Acute renal failure was reported more frequently in patients with advanced relapsed and refractory multiple myeloma who received KYPROLIS monotherapy. Monitor renal function with regular measurement of the serum creatinine and/or estimated creatinine clearance. Reduce or withhold dose as appropriate.
Tumor Lysis Syndrome

Cases of Tumor Lysis Syndrome (TLS), including fatal outcomes, have occurred in patients receiving KYPROLIS. Patients with multiple myeloma and a high tumor burden should be considered at greater risk for TLS. Adequate hydration is required prior to each dose in Cycle 1, and in subsequent cycles as needed. Consider uric acid lowering drugs in patients at risk for TLS. Monitor for evidence of TLS during treatment and manage promptly. Withhold KYPROLIS until TLS is resolved.
Pulmonary Toxicity

Acute Respiratory Distress Syndrome (ARDS), acute respiratory failure, and acute diffuse infiltrative pulmonary disease such as pneumonitis and interstitial lung disease have occurred in patients receiving KYPROLIS. Some events have been fatal. In the event of drug-induced pulmonary toxicity, discontinue KYPROLIS.
Pulmonary Hypertension

Pulmonary arterial hypertension (PAH) was reported in patients treated with KYPROLIS. Evaluate with cardiac imaging and/or other tests as indicated. Withhold KYPROLIS for PAH until resolved or returned to baseline and consider whether to restart KYPROLIS based on a benefit/risk assessment.
Dyspnea

Dyspnea was reported in patients treated with KYPROLIS. Evaluate dyspnea to exclude cardiopulmonary conditions including cardiac failure and pulmonary syndromes. Stop KYPROLIS for Grade 3 or 4 dyspnea until resolved or returned to baseline. Consider whether to restart KYPROLIS based on a benefit/risk assessment.
Hypertension

Hypertension, including hypertensive crisis and hypertensive emergency, has been observed with KYPROLIS. Some of these events have been fatal. Monitor blood pressure regularly in all patients. If hypertension cannot be adequately controlled, withhold KYPROLIS and evaluate. Consider whether to restart KYPROLIS based on a benefit/risk assessment.
Venous Thrombosis

Venous thromboembolic events (including deep venous thrombosis and pulmonary embolism) have been observed with KYPROLIS. Thromboprophylaxis is recommended for patients being treated with the combination of KYPROLIS with dexamethasone or with lenalidomide plus dexamethasone. The thromboprophylaxis regimen should be based on an assessment of the patient’s underlying risks.
Patients using oral contraceptives or a hormonal method of contraception associated with a risk of thrombosis should consider an alternative method of effective contraception during treatment with KYPROLIS in combination with dexamethasone or lenalidomide plus dexamethasone.
Infusion Reactions

Infusion reactions, including life-threatening reactions, have occurred in patients receiving KYPROLIS. Symptoms include fever, chills, arthralgia, myalgia, facial flushing, facial edema, vomiting, weakness, shortness of breath, hypotension, syncope, chest tightness, or angina. These reactions can occur immediately following or up to 24 hours after administration of KYPROLIS. Premedicate with dexamethasone to reduce the incidence and severity of infusion reactions. Inform patients of the risk and of symptoms of an infusion reaction and to contact a physician immediately if they occur.
Thrombocytopenia

KYPROLIS causes thrombocytopenia with recovery to baseline platelet count usually by the start of the next cycle. Thrombocytopenia was reported in patients receiving KYPROLIS. Monitor platelet counts frequently during treatment with KYPROLIS. Reduce or withhold dose as appropriate.
Hepatic Toxicity and Hepatic Failure

Cases of hepatic failure, including fatal cases, have been reported during treatment with KYPROLIS. KYPROLIS can cause increased serum transaminases. Monitor liver enzymes regularly regardless of baseline values. Reduce or withhold dose as appropriate.
Thrombotic Microangiopathy

Cases of thrombotic microangiopathy, including thrombotic thrombocytopenic purpura/hemolytic uremic syndrome (TTP/HUS), including fatal outcome have occurred in patients receiving KYPROLIS. Monitor for signs and symptoms of TTP/HUS. Discontinue KYPROLIS if diagnosis is suspected. If the diagnosis of TTP/HUS is excluded, KYPROLIS may be restarted. The safety of reinitiating KYPROLIS therapy in patients previously experiencing TTP/HUS is not known.
Posterior Reversible Encephalopathy Syndrome (PRES)

Cases of PRES have occurred in patients receiving KYPROLIS. PRES was formerly known as Reversible Posterior Leukoencephalopathy Syndrome. Consider a neuroradiological imaging (MRI) for onset of visual or neurological symptoms. Discontinue KYPROLIS if PRES is suspected and evaluate. The safety of reinitiating KYPROLIS therapy in patients previously experiencing PRES is not known.
Embryo-fetal Toxicity

KYPROLIS can cause fetal harm when administered to a pregnant woman based on its mechanism of action and findings in animals.
Females of reproductive potential should be advised to avoid becoming pregnant while being treated with KYPROLIS. Males of reproductive potential should be advised to avoid fathering a child while being treated with KYPROLIS. If this drug is used during pregnancy, or if pregnancy occurs while taking this drug, the patient should be apprised of the potential hazard to the fetus.
ADVERSE REACTIONS

The most common adverse events occurring in at least 20 percent of patients treated with KYPROLIS in the combination therapy trials: anemia, neutropenia, diarrhea, dyspnea, fatigue, thrombocytopenia, pyrexia, insomnia, muscle spasm, cough, upper respiratory tract infection, hypokalemia.
The most common adverse events occurring in at least 20 percent of patients treated with KYPROLIS in monotherapy trials: anemia, fatigue, thrombocytopenia, nausea, pyrexia, dyspnea, diarrhea, headache, cough, edema peripheral.
Please see full Prescribing Information at www.kyprolis.com.

Endocyte to Announce Updated Data on EC1456 and EC1169 at the 2016 American Society of Clinical Oncology (ASCO) Annual Meeting

On May 26, 2016 Endocyte, Inc. (NASDAQ:ECYT), a leader in developing targeted small molecule drug conjugates (SMDCs) and companion imaging agents for personalized therapy, reported that two posters will be presented on its lead, clinical-stage assets, EC1456 and EC1169, at the 2016 American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper) Annual Meeting being held June 3 – 7, 2016, in Chicago (Press release, Endocyte, MAY 26, 2016, View Source [SID:1234512816]).

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Updated data will be presented on EC1456-01, a phase 1 dose escalation study in patients with advanced solid tumors who were imaged to assess folate receptor expression with 99mTc-etarfolatide (FR expression not an eligibility criteria). Findings include:

EC1456 is generally well tolerated in previously treated cancer patients at the doses administered to date. Fifty-eight patients have been treated and are evaluable for cycle 1 toxicity. To date, the maximum tolerated dose (MTD) has not been determined. Dose escalation is ongoing at 12.5 mg/m2 on the weekly (QW) schedule and at 7.5 mg/m2 on the twice weekly (BIW) schedule.
Anti-tumor activity is suggested with lesion-level responses and 20 patients demonstrating stable disease (SD) and SD ≥ 3 months being observed in 5 BIW patients and 5 QW patients.
An update also will be provided for EC1169-01, a phase 1 dose escalation study in patients with metastatic, castration-resistant prostate cancer (mCRPC) who failed prior chemotherapy. All patients were imaged to assess PSMA expression with 99mTc-EC0652 (PSMA expression not an eligibility criteria). Findings include:

99mTC-EC0652 uptake was observed in all patients in both bone and soft tissue lesions. Both positive and negative lesion uptake was observed.
EC1169 is well tolerated in mCRPC patients at the doses administered to date. Twenty-eight patients have been treated and are evaluable for cycle 1 toxicity (TIW: 5 patients; QW: 23 patients). To date, the MTD has not been determined. Dose escalation is ongoing at 6.5 mg/m2 on the QW schedule.
Anti-tumor activity is suggested with lesion-level reductions. Furthermore, fifteen patients have demonstrated stable disease, and 2 patients have demonstrated a ≥50% max decline in PSA.
The posters will be available on Endocyte’s website following presentation at the conference.

Presentations are as follows:

Abstract #: 2585
Title: A phase 1 dose-escalation study of the folic acid-tubulysin small molecule drug conjugate (SMDC) folate-tubulysin EC1456 in advanced cancer patients
Presenter: Jasgit C. Sachdev, MD, Scottsdale Healthcare
When: Sunday, June 5, 8 a.m. – 11:30 a.m. EDT
Session Title: Developmental Therapeutics – Clinical Pharmacology and Experimental Therapeutics
Location: Hall A

Abstract #: 2586
Title: Phase 1 study of the PSMA-targeted tubulysin small-molecule drug conjugate EC1169 in patients with metastatic castrate-resistant prostate cancer (mCRPC)
Presenter: Michael J. Morris, MD, Memorial Sloan Kettering Cancer Center and Weill Cornell Medical College
When: Sunday, June 5, 8 a.m. – 11:30 a.m. EDT
Session Title: Developmental Therapeutics – Clinical Pharmacology and Experimental Therapeutics
Location: Hall A

About EC1456

EC1456 is an investigational, proprietary, injectable SMDC consisting of folate (vitamin B9) linked to a potent cytotoxic agent, tubulysin B hydrazide (TubBH). EC1456 is wholly owned by Endocyte. TubBH is a member of the tubulysin class of anti-neoplastic agents that inhibit the polymerization of tubulin into microtubules, a critical component during cell division. The targeting ligand folate, essential for cell division, has been investigated with vintafolide. EC1456 is currently being evaluated in a phase 1 study in patients with advanced solid tumors (ClinicalTrials.gov Identifier: NCT01999738).

About EC1169

EC1169 is an investigational, proprietary, injectable SMDC consisting of a PSMA targeting ligand (DUPA analog) linked to a potent cytotoxic agent, tubulysin B hydrazide (TubBH). EC1169 is wholly owned by Endocyte. TubBH is a member of the tubulysin class of anti-neoplastic agents that inhibit the polymerization of tubulin into microtubules, a critical component during cell division. EC1169 is currently being evaluated in a phase 1 study in patients with metastatic, castration-resistant prostate cancer (mCRPC) (ClinicalTrials.gov Identifier: NCT02202447).