Merrimack Pharmaceuticals Announces Expansion of MM-398 (nal-IRI) Imaging Study to Patients with Metastatic Breast Cancer

On June 11, 2015 Merrimack reported the initiation of clinical imaging assessing the use of a potential marker for delivery of MM-398 (irinotecan liposome injection), also known as "nal-IRI," to metastatic breast cancer (Press release, Merrimack, JUN 11, 2015, View Source [SID:1234505397]). This study is an expansion of a Phase 1 pilot study which assessed the feasibility of using ferumoxytol*, an iron oxide nanoparticle, to act as a marker for MM-398 tumor response prediction. The study will now enroll patients who have metastatic breast cancer which is either hormone receptor-positive, triple-negative, or where active brain metastases are present.

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"We were encouraged by the results of the initial pilot phase of the study, particularly the data that suggest a relationship between high levels of ferumoxytol uptake and shrinkage of tumor lesions after MM-398 treatment," said Dr. Jasgit Sachdev, MD, Virginia G Piper Cancer Center. "We are excited to continue to evaluate the activity of MM-398 and the predictive value of this imaging approach in additional patients with metastatic breast cancer."

The data from the initial pilot study (n=31 lesions comprising 9 patients) showed a relationship between ferumoxytol levels in individual tumor lesions, as measured using magnetic resonance imaging, and corresponding change in individual tumor lesion size following treatment with MM-398. Results observed in several patients with metastatic breast cancer in the pilot study warranted further expansion of the study to additional patients in this population. Adverse events from MM-398 therapy were consistent with previous studies. Reported grade 3 and above adverse events related to MM-398 treatment included diarrhea, hypokalemia, abdominal pain, anemia, nausea and neutropenia.

"We look forward to expanding this study and aim to use it to support our biomarker hypothesis and further our strategy to use diagnostic imaging to identify the patients who are most likely to derive benefit from treatment with MM-398," said Bart Hendriks, Ph.D., Director of Imaging Diagnostics at Merrimack.

As part of this expansion, 30 patients with metastatic breast cancer will be imaged with ferumoxytol followed by treatment with MM-398. Ten patients will be enrolled in each of three cohorts as follows: ER and/or PR-positive metastatic breast cancer, triple-negative metastatic breast cancer or metastatic breast cancer with active brain metastases. Eligible patients for the trial must have received less than four prior lines of chemotherapy for the treatment of metastatic disease. The primary objectives of this study are to investigate the feasibility of ferumoxytol quantitation in tumor lesions and to characterize the relationship between ferumoxytol uptake in the tumor and tumor response to MM-398 in patients with advanced metastatic breast cancer. Merrimack plans to conduct the trial at multiple sites in the United States. The Virginia G Piper Cancer Center in Scottsdale, Arizona is now open to screen patients. For more information, please visit clinicaltrials.gov (Identifier: NCT01770353).

About MM-398

MM-398 (irinotecan liposome injection), is an encapsulation of irinotecan in a long-circulating liposomal formulation. The activated form of irinotecan is SN-38, which functions by inhibiting topoisomerase I (an essential enzyme involved in DNA transcription and replication) and promoting cell death. Merrimack and Baxter International’s biopharmaceutical business (NYSE: BAX) have an exclusive licensing agreement to develop and commercialize MM-398 outside of the United States. PharmaEngine, Inc. (Taipei, Taiwan) holds the rights to commercialize MM-398 in Taiwan.

8-K – Current report

On June 11, 2015, Cellectar Biosciences reported that, after review of the company’s investigational new drug (IND) application, the U.S. Food and Drug Administration (FDA) has determined that Cellectar’s tumor margin illumination agent, CLR1502, will be evaluated as a combination product and assigned to the Center for Devices and Radiological Health (CDRH) (Filing, 8-K, Cellectar Biosciences, JUN 11, 2015, View Source [SID:1234505396]). As a result of this classification, the FDA has advised Cellectar that it will need to submit a new investigational application for the combination product prior to initiating its planned proof-of-concept trial in breast cancer surgery.

"Our tumor illumination agent shares similar spectral qualities with indocyanine green (ICG), a fluorescent dye commonly used in medical diagnostics, and can therefore use several commercially available fluorescent imaging devices. Current labeling for such devices is limited to FDA approved applications such as cardiac, circulatory, hepatic and ophthalmic conditions," said Dr. Simon Pedder, president and chief executive officer of Cellectar Biosciences. "Because of the groundbreaking nature of our overall technology and the potential for an agent like CLR1502 to dramatically expand the utility of such imaging devices, we appreciate the agency’s perspective and current interest in evaluating CLR1502 in combination with a light source technology. As previously disclosed, in the course of our discussions FDA regarding the CLR1502 registration program, the FDA has stressed that a combination product designation is not binding, can be revised later in our development program, and that we are not necessarily precluded from filing a standalone NDA in the future."

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About CLR1502

CLR1502 is a small-molecule, broad-spectrum, cancer-targeted, non-radioactive optical imaging agent developed by Cellectar to be the first of its kind for broad spectrum intraoperative tumor margin illumination and non-invasive tumor imaging. CLR1502 is comprised of a proprietary phospholipid ether (PLE) analog, acting as a cancer-targeted delivery and retention vehicle attached to a fluorophore to enable real-time visualization of malignant tissue under near-infrared light.

CLR1502 is being developed for intraoperative imaging of cancer that will aid in the identification of malignant tissue during diagnostic, staging, debulking and curative cancer surgeries. In particular, the potential of CLR1502 in tumor margin illumination during oncologic resections raises the possibility that this operative aid may improve surgical outcomes.

AVEO Announces FDA Update for Tivozanib in Colorectal Cancer

On June 11, 2015 AVEO Oncology reported that it has received written feedback from the U.S. Food and Drug Administration regarding a potential pivotal study for tivozanib in the treatment of NRP-1 low colorectal cancer (CRC) (Press release, AVEO, JUN 11, 2015, View Source;p=RssLanding&cat=news&id=2058718 [SID:1234505395]). Tivozanib is an oral, potent, selective inhibitor of vascular endothelial growth factor (VEGF) with a long half-life and activity against all three VEGF receptors.

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AVEO recently presented results from the BATON-CRC study, a 265 patient randomized trial exploring the combination of mFOLFOX6 and tivozanib or bevacizumab as first-line treatment in patients with advanced metastatic CRC, at the 2015 American Association for Cancer Research (AACR) (Free AACR Whitepaper) Tumor Angiogenesis and Vascular Normalization Conference. Among the predefined biomarkers explored in this study, neuropilin-1 (NRP-1), a signaling protein known to bind to VEGF-A in serum, was found to be a potential prognostic marker for angiogenesis inhibitor activity and may be predictive of tivozanib activity relative to bevacizumab.

Results from this study and the Company’s ongoing assay development efforts were presented to the FDA. Updated analyses from the Company’s assay development efforts, which are similar to those presented at the AACR (Free AACR Whitepaper) conference, will be presented at the upcoming European Society of Medical Oncology (ESMO) (Free ESMO Whitepaper) 17th World Congress on Gastrointestinal Cancer taking place July 1-4, 2015 in Barcelona Spain.

In response to questions from AVEO regarding a proposed pivotal phase 3 trial of tivozanib in CRC, the FDA suggested that the Company continue work on the development of its biomarker assay to address variability between assays presented, and that, at present, "insufficient data exists to determine the appropriateness of this [NRP-1 low] subgroup" for the proposed phase 3 study. This feedback is consistent with the Company’s current clinical strategy and discussions with cancer research cooperative groups. As such, AVEO plans to evaluate options to confirm the activity of tivozanib and FOLFOX in NRP-1 low CRC through a prospectively defined, randomized Phase 2 study, while continuing to work on the development of a commercially viable assay.

"NRP-1 expression is a biomarker of growing interest for malignancies treated with angiogenesis inhibitors," said Michael Bailey, president and chief executive officer of AVEO. "As part of our effort to develop a commercial companion diagnostic, we continue to evaluate alternative NRP-1 assays. Feedback from the FDA reinforces the importance of these ongoing efforts prior to embarking on a pivotal trial. We look forward to continuing our dialogue with the Agency and cooperative groups toward the design and potential conduct of an appropriate confirmatory study and the development of a companion diagnostic."

Bristol-Myers Squibb Demonstrates Commitment to Hematology and Advancing Research and Development Across Multiple Blood Cancers Through Immuno-Oncology Leadership at the 20th Congress of the European Hematology Association

On June 11, 2015 Bristol-Myers Squibb reported the presentation of clinical research from its hematology portfolio at the 20th Congress of the European Hematology Association (EHA) (Free EHA Whitepaper) in Vienna, Austria from June 11-14 (Press release, Bristol-Myers Squibb, JUN 11, 2015, View Source [SID:1234505393]). Bristol-Myers Squibb will present data for elotuzumab, an investigational immunostimulatory antibody, in relapsed or refractory multiple myeloma; Opdivo (nivolumab), in patients with relapsed or refractory lymphoid malignancies; and Sprycel (dasatinib), in chronic myeloid leukemia.

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Data to be presented at EHA (Free EHA Whitepaper) exemplify Bristol-Myers Squibb’s commitment to advancing the treatment of blood cancers through its experience in hematology and its transformative science of Immuno-Oncology.

Key oral presentations include:

ELOQUENT-2: A Phase 3, open-label study [Abstract #S471] comparing elotuzumab in combination with lenalidomide and dexamethasone (ELd) versus lenalidomide and dexamethasone alone (Ld) in patients with relapsed or refractory multiple myeloma, will be featured in the EHA (Free EHA Whitepaper) press briefing on Friday, June 12 at 8:30 a.m. CEST and will be presented during the Presidential Symposium, also on June 12, at 3:45 p.m. CEST. The ELOQUENT-2 study was published in the New England Journal of Medicine on June 2.

Study 009: A Phase 2, open-label study [Abstract #S103] comparing elotuzumab in combination with bortezomib (a proteasome inhibitor) and dexamethasone versus bortezomib and dexamethasone in patients with relapsed or refractory multiple myeloma will be presented in an oral session on June 12 at 12:00 p.m. CEST.

PREAMBLE: A preliminary analysis of an ongoing, multinational, observational study [Abstract #S148] evaluating the real-world clinical effectiveness of standard treatments, including immunomodulatory drugs (IMiDs) and proteasome inhibitors (PIs), in patients with relapsed or refractory multiple myeloma will be presented in an oral session on June 12 at 12:00 p.m. CEST.

CheckMate -039: Updated data from a Phase 1 study [Abstract #S808] evaluating the safety, tolerability and potential efficacy of Opdivo in several hematologic malignancies, including classical Hodgkin Lymphoma will be presented in an oral session on Sunday, June 14 at 8:45 a.m. CEST.

"Bristol-Myers Squibb is leveraging its broad experience in oncology and leading Immuno-Oncology science to develop a portfolio of innovative therapies, including a novel modality for multiple myeloma, because we believe patients with blood cancers deserve more," said Michael Giordano, senior vice president, Head of Development, Oncology, Bristol-Myers Squibb. "These data at EHA (Free EHA Whitepaper) illustrate our commitment to transforming survival expectations for more patients with a variety of hematologic malignancies."

About Elotuzumab

Elotuzumab is an investigational immunostimulatory antibody targeted against Signaling Lymphocyte Activation Molecule (SLAMF7), a cell-surface glycoprotein that is highly and uniformly expressed on myeloma cells and Natural Killer (NK) cells, but is not detected on normal solid tissues or on hematopoietic stem cells. Elotuzumab is being investigated to determine whether the compound may selectively target myeloma cells. It is believed that elotuzumab works through a dual mechanism of action: binding to SLAMF7 on NK cells, directly activating them and binding to SLAMF7 on myeloma cells, flagging them for NK cell recognition and destruction.

In May 2014, the U.S. Food and Drug Administration (FDA) granted elotuzumab Breakthrough Therapy Designation for use in combination with one of the chemotherapy treatments for multiple myeloma (lenalidomide, used in combination with dexamethasone) in patients who have received one or more prior treatments. Elotuzumab is an investigational compound, and its safety and efficacy have not been evaluated by the FDA or any other health authority.

Bristol-Myers Squibb and AbbVie are co-developing elotuzumab, with Bristol-Myers Squibb solely responsible for commercial activities.

About Opdivo

Bristol-Myers Squibb has a broad, global development program to study Opdivo in multiple tumor types consisting of more than 50 trials – as monotherapy or in combination with other therapies – in which more than 8,000 patients have been enrolled worldwide.

In May 2014, the FDA granted Opdivo Breakthrough Therapy Designation for the treatment of patients with Hodgkin Lymphoma after failure of autologous stem cell transplant and brentuximab. Opdivo became the first PD-1 immune checkpoint inhibitor to receive regulatory approval anywhere in the world on July 4, 2014 when Ono Pharmaceutical Co. announced that it received manufacturing and marketing approval in Japan for the treatment of patients with unresectable melanoma. In the U.S., the (FDA) granted its first approval for Opdivo for the treatment of patients with unresectable or metastatic melanoma and disease progression following Yervoy (ipilimumab) and, if BRAF V600 mutation positive, a BRAF inhibitor. On March 4, 2015, Opdivo received its second FDA approval for the treatment of patients with metastatic squamous non-small cell lung cancer with progression on or after platinum-based chemotherapy.

OPDIVO (nivolumab) IMPORTANT SAFETY INFORMATION

Immune-Mediated Pneumonitis

Severe pneumonitis or interstitial lung disease, including fatal cases, occurred with OPDIVO treatment. Across the clinical trial experience in 691 patients with solid tumors, fatal immune-mediated pneumonitis occurred in 0.7% (5/691) of patients receiving OPDIVO; no cases occurred in Trial 1 or Trial 3. In Trial 1, pneumonitis, including interstitial lung disease, occurred in 3.4% (9/268) of patients receiving OPDIVO and none of the 102 patients receiving chemotherapy. Immune-mediated pneumonitis occurred in 2.2% (6/268) of patients receiving OPDIVO; one with Grade 3 and five with Grade 2. In Trial 3, immune-mediated pneumonitis occurred in 6% (7/117) of patients receiving OPDIVO, including, five Grade 3 and two Grade 2 cases. Monitor patients for signs and symptoms of pneumonitis. Administer corticosteroids for Grade 2 or greater pneumonitis. Permanently discontinue OPDIVO for Grade 3 or 4 and withhold OPDIVO until resolution for Grade 2.

Immune-Mediated Colitis

In Trial 1, diarrhea or colitis occurred in 21% (57/268) of patients receiving OPDIVO and 18% (18/102) of patients receiving chemotherapy. Immune-mediated colitis occurred in 2.2% (6/268) of patients receiving OPDIVO; five with Grade 3 and one with Grade 2. In Trial 3, diarrhea occurred in 21% (24/117) of patients receiving OPDIVO. Grade 3 immune-mediated colitis occurred in 0.9% (1/117) of patients. Monitor patients for immune-mediated colitis. Administer corticosteroids for Grade 2 (of more than 5 days duration), 3, or 4 colitis. Withhold OPDIVO for Grade 2 or 3. Permanently discontinue OPDIVO for Grade 4 colitis or recurrent colitis upon restarting OPDIVO.

Immune-Mediated Hepatitis

In Trial 1, there was an increased incidence of liver test abnormalities in the OPDIVO-treated group as compared to the chemotherapy-treated group, with increases in AST (28% vs 12%), alkaline phosphatase (22% vs 13%), ALT (16% vs 5%), and total bilirubin (9% vs 0). Immune-mediated hepatitis occurred in 1.1% (3/268) of patients receiving OPDIVO; two with Grade 3 and one with Grade 2. In Trial 3, the incidences of increased liver test values were AST (16%), alkaline phosphatase (14%), ALT (12%), and total bilirubin (2.7%). Monitor patients for abnormal liver tests prior to and periodically during treatment. Administer corticosteroids for Grade 2 or greater transaminase elevations. Withhold OPDIVO for Grade 2 and permanently discontinue OPDIVO for Grade 3 or 4 immune-mediated hepatitis.

Immune-Mediated Nephritis and Renal Dysfunction

In Trial 1, there was an increased incidence of elevated creatinine in the OPDIVO-treated group as compared to the chemotherapy-treated group (13% vs 9%). Grade 2 or 3 immune-mediated nephritis or renal dysfunction occurred in 0.7% (2/268) of patients. In Trial 3, the incidence of elevated creatinine was 22%. Immune-mediated renal dysfunction (Grade 2) occurred in 0.9% (1/117) of patients. Monitor patients for elevated serum creatinine prior to and periodically during treatment. For Grade 2 or 3 serum creatinine elevation, withhold OPDIVO and administer corticosteroids; if worsening or no improvement occurs, permanently discontinue OPDIVO. Administer corticosteroids for Grade 4 serum creatinine elevation and permanently discontinue OPDIVO.

Immune-Mediated Hypothyroidism and Hyperthyroidism

In Trial 1, Grade 1 or 2 hypothyroidism occurred in 8% (21/268) of patients receiving OPDIVO and none of the 102 patients receiving chemotherapy. Grade 1 or 2 hyperthyroidism occurred in 3% (8/268) of patients receiving OPDIVO and 1% (1/102) of patients receiving chemotherapy. In Trial 3, hypothyroidism occurred in 4.3% (5/117) of patients receiving OPDIVO. Hyperthyroidism occurred in 1.7% (2/117) of patients, including one Grade 2 case. Monitor thyroid function prior to and periodically during treatment. Administer hormone replacement therapy for hypothyroidism. Initiate medical management for control of hyperthyroidism.

Other Immune-Mediated Adverse Reactions

In Trial 1 and 3 (n=385), the following clinically significant immune-mediated adverse reactions occurred in <2% of OPDIVO-treated patients: adrenal insufficiency, uveitis, pancreatitis, facial and abducens nerve paresis, demyeliniation, autoimmune neuropathy, motor dysfunction, and vasculitis. Across clinical trials of OPDIVO administered at doses 3 mg/kg and 10 mg/kg, additional clinically significant, immune-mediated adverse reactions were identified: hypophysitis, diabetic ketoacidosis, hypopituitarism, Guillain-Barré syndrome, and myasthenic syndrome. Based on the severity of adverse reaction, withhold OPDIVO, administer high-dose corticosteroids, and, if appropriate, initiate hormone- replacement therapy.

Embryofetal Toxicity

Based on its mechanism of action, OPDIVO can cause fetal harm when administered to a pregnant woman. Advise pregnant women of the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during treatment with OPDIVO and for at least 5 months after the last dose of OPDIVO.

Lactation

It is not known whether OPDIVO is present in human milk. Because many drugs, including antibodies, are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from OPDIVO, advise women to discontinue breastfeeding during treatment.

Serious Adverse Reactions

In Trial 1, serious adverse reactions occurred in 41% of patients receiving OPDIVO. Grade 3 and 4 adverse reactions occurred in 42% of patients receiving OPDIVO. The most frequent Grade 3 and 4 adverse drug reactions reported in 2% to <5% of patients receiving OPDIVO were abdominal pain, hyponatremia, increased aspartate aminotransferase, and increased lipase.

In Trial 3, serious adverse reactions occurred in 59% of patients receiving OPDIVO. The most frequent serious adverse drug reactions reported in ≥2% of patients were dyspnea, pneumonia, chronic obstructive pulmonary disease exacerbation, pneumonitis, hypercalcemia, pleural effusion, hemoptysis, and pain.

Common Adverse Reactions

The most common adverse reactions (≥20%) reported with OPDIVO in Trial 1 were rash (21%) and in Trial 3 were fatigue (50%), dyspnea (38%), musculoskeletal pain (36%), decreased appetite (35%), cough (32%), nausea (29%), and constipation (24%).
Please see U.S. Full Prescribing Information for OPDIVO.

About Sprycel

Sprycel is a prescription medicine used to treat adults who have newly diagnosed Philadelphia chromosome–positive (Ph+) chronic myeloid leukemia (CML) in chronic phase. The effectiveness of Sprycel in these patients is based on a study that measured two types of response to treatment (cytogenetic and molecular) by one year. The study is ongoing to find out how Sprycel works over a longer period of time. Sprycel is also indicated for adults with Ph+ CML who are no longer benefitting from, or did not tolerate, other treatment including Gleevec (imatinib mesylate).

SPRYCEL (dasatinib) INDICATIONS & IMPORTANT SAFETY INFORMATION

INDICATIONS

SPRYCEL (dasatinib) is indicated for the treatment of adults with:

Newly diagnosed Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in chronic phase. The effectiveness of SPRYCEL is based on cytogenetic and major molecular response rates. The trial is ongoing and further data will be required to determine long-term outcome

Chronic, accelerated, or myeloid or lymphoid blast phase Ph+ CML with resistance or intolerance to prior therapy including imatinib
Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) with resistance or intolerance to prior therapy

IMPORTANT SAFETY INFORMATION

Myelosuppression:

Treatment with SPRYCEL (dasatinib) can cause severe (NCI CTC Grade 3/4) thrombocytopenia, neutropenia, and anemia. Their occurrence is more frequent in patients with advanced phase CML or Ph+ ALL than in chronic phase CML. Myelosuppression was reported in patients with normal baseline laboratory values as well as in patients with pre-existing laboratory abnormalities.

Perform complete blood counts (CBCs) weekly for the first 2 months and then monthly thereafter, or as clinically indicated
Myelosuppression was generally reversible and usually managed by dose interruption, dose reduction, or discontinuation
Hematopoietic growth factor has been used in patients with resistant myelosuppression

Bleeding Related Events:

SPRYCEL caused platelet dysfunction in vitro and thrombocytopenia in humans. In all clinical trials, severe central nervous system (CNS) hemorrhage, including fatalities, occurred in 1% of patients receiving SPRYCEL. Severe gastrointestinal hemorrhage, including fatalities, occurred in 4% of patients and generally required treatment interruptions and transfusions. Other cases of severe hemorrhage occurred in 2% of patients.

Most bleeding events were associated with severe thrombocytopenia. Exercise caution in patients required to take medications that inhibit platelet function or anticoagulants

Fluid Retention:

SPRYCEL is associated with fluid retention. In clinical trials, fluid retention was severe in up to 10% of patients. Severe ascites, pulmonary edema, and generalized edema were each reported in ≤1% of patients.

Patients who develop symptoms suggestive of pleural effusion, such as dyspnea or dry cough, should be evaluated by chest X-ray
Severe pleural effusion may require thoracentesis and oxygen therapy
Fluid retention was typically managed by supportive care measures that included diuretics or short courses of steroids

QT Prolongation:

In vitro data suggest that SPRYCEL has the potential to prolong cardiac ventricular repolarization (QT interval).

In 865 patients with leukemia treated with SPRYCEL in five phase 2 single-arm studies, the maximum mean changes in QTcF (90% upper bound CI) from baseline ranged from 7.0 ms to 13.4 ms
In clinical trials of patients treated with SPRYCEL (N=2440), 16 patients (1%) had QTc prolongation as an adverse reaction. Twenty-two patients (1%) experienced a QTcF>500 ms
Administer SPRYCEL with caution to patients who have or may develop prolongation of QTc, including patients with hypokalemia, hypomagnesemia, or congenital long QT syndrome and patients taking antiarrhythmic drugs, other medicinal products that lead to QT prolongation, and cumulative high-dose anthracycline therapy
Correct hypokalemia or hypomagnesemia prior to SPRYCEL administration

Congestive Heart Failure, Left Ventricular Dysfunction, and Myocardial Infarction:

Cardiac adverse reactions were reported in 7% of 258 patients taking SPRYCEL, including 1.6% of patients with cardiomyopathy, heart failure congestive, diastolic dysfunction, fatal myocardial infarction, and left ventricular dysfunction.

Monitor patients for signs or symptoms consistent with cardiac dysfunction and treat appropriately

Pulmonary Arterial Hypertension (PAH):

SPRYCEL may increase the risk of developing PAH, which may occur any time after initiation, including after more than one year of treatment. Manifestations include dyspnea, fatigue, hypoxia, and fluid retention. PAH may be reversible on discontinuation of SPRYCEL.

Evaluate patients for signs and symptoms of underlying cardiopulmonary disease prior to initiating SPRYCEL and during treatment. If PAH is confirmed, SPRYCEL should be permanently discontinued

Use in Pregnancy:

SPRYCEL may cause fetal harm when administered to a pregnant woman. There are no adequate and well-controlled studies of SPRYCEL in pregnant women.

Women of childbearing potential should be advised of the potential hazard to the fetus and to avoid becoming pregnant when taking SPRYCEL

Nursing Mothers:

It is unknown whether SPRYCEL is excreted in human milk.

Because of the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue SPRYCEL

SPRYCEL is a CYP3A4 substrate and a weak time-dependent inhibitor of CYP3A4.

Drugs that may increase SPRYCEL plasma concentrations are:
CYP3A4 inhibitors: Concomitant use of SPRYCEL and drugs that inhibit CYP3A4 should be avoided. If administration of a potent CYP3A4 inhibitor cannot be avoided, close monitoring for toxicity and a SPRYCEL dose reduction should be considered

Strong CYP3A4 inhibitors (eg, ketoconazole, itraconazole, clarithromycin, atazanavir, indinavir, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole). If SPRYCEL must be administered with a strong CYP3A4 inhibitor, a dose decrease or temporary discontinuation should be considered
Grapefruit juice may also increase plasma concentrations of SPRYCEL and should be avoided

Drugs that may decrease SPRYCEL plasma concentrations are:
CYP3A4 inducers: If SPRYCEL must be administered with a CYP3A4 inducer, a dose increase in SPRYCEL should be considered

Strong CYP3A4 inducers (eg, dexamethasone, phenytoin, carbamazepine, rifampin, rifabutin, phenobarbital) should be avoided. Alternative agents with less enzyme induction potential should be considered. If the dose of SPRYCEL is increased, the patient should be monitored carefully for toxicity
St John’s Wort may decrease SPRYCEL plasma concentrations unpredictably and should be avoided

Antacids may decrease SPRYCEL drug levels. Simultaneous administration of SPRYCEL and antacids should be avoided. If antacid therapy is needed, the antacid dose should be administered at least 2 hours prior to or 2 hours after the dose of SPRYCEL

H2 antagonists/proton pump inhibitors (eg, famotidine and omeprazole): Long-term suppression of gastric acid secretion by use of H2 antagonists or proton pump inhibitors is likely to reduce SPRYCEL exposure. Therefore, concomitant use of H2 antagonists or proton pump inhibitors with SPRYCEL is not recommended

Drugs that may have their plasma concentration altered by SPRYCEL are:
CYP3A4 substrates (eg, simvastatin) with a narrow therapeutic index should be administered with caution in patients receiving SPRYCEL

Adverse Reactions:

The safety data reflect exposure to SPRYCEL in 258 patients with newly diagnosed chronic phase CML in a clinical trial (minimum of 36 months follow up; median duration of therapy was 37 months), and in 2182 patients with imatinib-resistant or -intolerant CML or Ph+ ALL in clinical trials (1520 patients had a minimum of 2 years follow up and 662 patients with chronic phase CML had a minimum of 60 months follow up).

The majority of SPRYCEL-treated patients experienced adverse reactions at some time. Patients aged 65 years and older are more likely to experience toxicity. In the newly diagnosed chronic phase CML trial, the cumulative discontinuation rate was 9% with a minimum of 36 months follow up. In patients resistant or intolerant to prior imatinib therapy, the discontinuation rate for SPRYCEL at 2 years for adverse reactions was: 15% of patients in chronic phase CML (all doses), 16% of patients in accelerated phase CML, 15% of patients in myeloid blast phase CML, 8% in lymphoid blast phase CML, and 8% in Ph+ ALL. In patients resistant or intolerant to prior imatinib therapy with chronic phase CML (minimum 60 months follow up), the rate of discontinuation for adverse reactions was 18% in patients treated with 100 mg once daily.

In newly diagnosed chronic phase CML patients:
The most frequently reported serious adverse reactions included pleural effusion (4%), hemorrhage (2%), congestive heart failure (1%), pulmonary hypertension (1%), and pyrexia (1%)

The most frequently reported adverse reactions (reported in ≥10% of patients) included myelosuppression, fluid retention events (pleural effusion and superficial localized edema), diarrhea, headache, musculoskeletal pain, rash, and nausea

Grade 3/4 laboratory abnormalities included neutropenia (24%), thrombocytopenia (19%), anemia (12%), hypophosphatemia (7%), hypocalcemia (3%), elevated bilirubin (1%), and elevated creatinine (1%)

In patients resistant or intolerant to prior imatinib therapy:
The most frequently reported serious adverse reactions included pleural effusion (11%), gastrointestinal bleeding (4%), febrile neutropenia (4%), dyspnea (3%), pneumonia (3%), pyrexia (3%), diarrhea (3%), infection (2%), congestive heart failure/cardiac dysfunction (2%), pericardial effusion (1%), and CNS hemorrhage (1%)

The most frequently reported adverse reactions (reported in ≥20% of patients) included myelosuppression, fluid retention events, diarrhea, headache, dyspnea, skin rash, fatigue, nausea, and hemorrhage

Grade 3/4 hematologic laboratory abnormalities in chronic phase CML patients resistant or intolerant to prior imatinib therapy who received SPRYCEL 100 mg once daily with a minimum follow up of 60 months included neutropenia (36%), thrombocytopenia (24%) and anemia (13%). Other grade 3/4 laboratory abnormalities included: hypophosphatemia (10%) and hypokalemia (2%)

Among chronic phase CML patients with resistance or intolerance to prior imatinib therapy, cumulative Grade 3 or 4 cytopenias were similar at 2 and 5 years including: neutropenia (36% vs 36%), thrombocytopenia (23% vs 24%), and anemia (13% vs 13%)
Grade 3/4 elevations of transaminase or bilirubin and Grade 3/4 hypocalcemia, hypokalemia, and hypophosphatemia were reported in patients with all phases of CML

Elevations in transaminase or bilirubin were usually managed with dose reduction or interruption

Patients developing Grade 3/4 hypocalcemia during the course of SPRYCEL therapy often had recovery with oral calcium supplementation

BIND Therapeutics and Macrophage Therapeutics Announce Collaboration to Engineer CD206 Targeted Accurin™ Nanoparticle Using Manocept™ Macrophage Targeting Platform

On June 11, 2015 BIND Therapeutics and Macrophage Therapeutics, a subsidiary of Navidea Biopharmaceuticals reported they have entered into a research collaboration to engineer Accurins with the Manocept targeting platform that enables selective, efficient binding to CD206 positive disease-associated macrophages (Press release, BIND Therapeutics, JUN 11, 2015, View Source [SID:1234505392]). Upon achievement of proof-of-concept, the companies anticipate expanding the collaboration to develop Manocept-linked Accurins as a novel, potent approach to impact the tumor microenvironment which, in many forms of cancer, is a barrier to immune effector cells.

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"This collaboration represents a potentially significant advance in the evolution of our platform as we develop Accurins with novel targeting ligands," said Andrew Hirsch, president and chief executive officer of BIND Therapeutics. "The modular nature of our platform offers multiple therapeutic possibilities, and our collaboration with Macrophage Therapeutics may enable the development of Accurins that target activated macrophages, which in cancer, help create an immunosuppressive microenvironment. We believe the clinically validated Manocept platform, with its unique ability to seek out activated macrophages, fits into our vision to engineer Accurins that have a profound impact on the treatment of diseases, including our current focus in cancer."

Disease-associated macrophages generally play a pro-tumoral role and are immunosuppressive, preventing the immune system from mounting an attack on tumor cells. Based on the expression of CD206 mannose receptors on disease-associated macrophages, BIND and Macrophage plan to conduct joint research to develop a CD206 targeted Accurin nanoparticle that is capable of concentrating various therapeutic payloads to the tumor microenvironment.

"We are pleased to work with BIND Therapeutics to explore the therapeutic potential of our two complementary technology platforms," said Michael M. Goldberg, M.D., CEO of Macrophage Therapeutics and Director of Navidea. "The Manocept platform is the basis for the FDA-approved CD206 targeted sentinel lymph node detection agent, Lymphoseek (technetium Tc 99m tilmanocept) injection. Coupled with BIND’s specifically engineered Accurins that concentrate therapeutic payloads to extracellular and intracellular compartments, with a tunable controlled-release profile, we are optimistic that we can create a wide range of therapeutic applications."

"It is well-established that macrophages play an important role in many disease states but it has proven difficult to selectively target and alter macrophages that play a key role in disease progression," said Hagop Youssoufian, M.Sc., M.D., chief medical officer at BIND Therapeutics. "By coupling Accurins with Macrophage’s well-credentialed CD206 targeting ligand, we may be able to treat macrophage-mediated diseases through increased uptake, and concentration, of targeted therapeutic payloads in the tumor microenvironment. BIND’s Medicinal Nanoengineering platform is able to combine multiple molecular components into a targeted, long-circulating Accurin. An Accurin nanoparticle that binds to CD206 positive macrophages could be a valuable asset in the armament against multiple cancers and disease states."

"The collaboration furthers our vision to develop therapeutic applications of the Manocept platform through strategic partnerships," said Rick Gonzalez, president and CEO of Navidea. "In collaborating with BIND, we will be able to leverage their accomplished R&D team who has strong track record for advancing targeted nanoparticles from concept into the clinic."

About Accurins

Accurins, a new class of targeted therapeutics developed using BIND’s Medicinal Nanoengineering platform, are nanoparticles engineered to have a profound impact on the treatment of disease. The elegant and novel design of Accurins allow for prolonged circulation, controlled and tunable release and selective targeting of a therapeutic payload to diseased tissue or cells while avoiding immune surveillance detection and systemic toxicities.

Accurins can be engineered for multiple therapeutic applications and have the potential to integrate numerous payloads, including highly potent drugs with mechanism-based toxicities that limit therapeutic benefit, DNA, RNA, proteins and immunotherapy agents. This attribute enables Accurins to target multiple diseases, including cancer, inflammatory, vascular, and infectious disease.

About Manocept CD206 Targeting Platform for Therapeutics Development

Manocept CD206 Targeting Platform is a proprietary mannose-containing, receptor-directed technology platform designed to engineer novel, synthetic receptor targeted imaging agents and therapeutics for cancer and other diseases. Manocept’s unique structural and molecular properties enable the design of novel immuno-constructs that selectively target and bind to CD206 (mannose receptor) and other C-type Lectins found on activated, disease-associated macrophages and tumor associated macrophages (TAMs). The Manocept CD206 Targeting Platform provides a novel and valuable approach to the design of drug molecules targeting CD206 disease-associated macrophages for therapeutic purposes.

About Lymphoseek

Lymphoseek (technetium Tc 99m tilmanocept) injection is the first and only FDA-approved receptor-targeted lymphatic mapping agent. It is a novel, receptor-targeted, small-molecule radiopharmaceutical used in the evaluation of lymphatic basins that may have cancer involvement in patients. Lymphoseek is designed for the precise identification of lymph nodes that drain from a primary tumor, which have the highest probability of harboring cancer. Lymphoseek is approved by the U.S. Food and Drug Administration (FDA) for use in solid tumor cancers where lymphatic mapping is a component of surgical management and for guiding sentinel lymph node biopsy in patients with clinically node negative breast cancer, melanoma or squamous cell carcinoma of the oral cavity. Lymphoseek has also received European approval in imaging and intraoperative detection of sentinel lymph nodes in patients with melanoma, breast cancer or localized squamous cell carcinoma of the oral cavity.

Accurate diagnostic evaluation of cancer is critical, as it guides therapy decisions and determines patient prognosis and risk of recurrence. Overall in the U.S., solid tumor cancers may represent up to 1.2 million cases per year. The sentinel node label in the U.S. and Europe may address approximately 235,000 new cases of breast cancer, 76,000 new cases of melanoma and 45,000 new cases of head and neck/oral cancer in the U.S., and approximately 367,000 new cases of breast cancer, 83,000 new cases of melanoma and 55,000 new cases of head and neck/oral cancer diagnosed in Europe annually.

Lymphoseek Indication and Important Safety Information

Lymphoseek is a radioactive diagnostic agent indicated with or without scintigraphic imaging for:

Lymphatic mapping using a handheld gamma counter to locate lymph nodes draining a primary tumor site in patients with solid tumors for which this procedure is a component of intraoperative management.
Guiding sentinel lymph node biopsy using a handheld gamma counter in patients with clinically node negative squamous cell carcinoma of the oral cavity, breast cancer or melanoma.
Important Safety Information

In clinical trials with Lymphoseek, no serious hypersensitivity reactions were reported, however Lymphoseek may pose a risk of such reactions due to its chemical similarity to dextran. Serious hypersensitivity reactions have been associated with dextran and modified forms of dextran (such as iron dextran drugs).

Prior to the administration of Lymphoseek, patients should be asked about previous hypersensitivity reactions to drugs, in particular dextran and modified forms of dextran. Resuscitation equipment and trained personnel should be available at the time of Lymphoseek administration, and patients observed for signs or symptoms of hypersensitivity following injection.

Any radiation-emitting product may increase the risk for cancer. Adhere to dose recommendations and ensure safe handling to minimize the risk for excessive radiation exposure to patients or health care workers.

In clinical trials, no patients experienced serious adverse reactions and the most common adverse reactions were injection site irritation and/or pain ( < 1%).