Zymeworks Submits Investigational New Drug (IND) Application for ZW49 and Presents IND-Enabling Studies at the San Antonio Breast Cancer Symposium

On December 8, 2018 Zymeworks Inc. (NYSE/TSX: ZYME), a clinical-stage biopharmaceutical company developing multifunctional therapeutics, reported IND-enabling data for ZW49, a novel biparatopic HER2-targeted ADC, at the San Antonio Breast Cancer Symposium in San Antonio, TX (Press release, Zymeworks, DEC 8, 2018, View Source [SID1234531961]).

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"These data highlight the potential efficacy of ZW49 versus leading HER2 ADCs and demonstrate the power of combining our therapeutic platforms to achieve greater efficacy and tolerability, thereby increasing the therapeutic window," said Ali Tehrani, Ph.D., President and CEO of Zymeworks. "With the recent submission of our IND for ZW49 we are pleased with the speed and trajectory of ZW49’s development and look forward to starting clinical trials in early 2019."

ZW49 is a HER2-targeted bispecific ADC that capitalizes on the unique geometry and antibody framework of Zymeworks’ lead clinical candidate, ZW25, and is armed with the Company’s proprietary ZymeLink-cytotoxic payload. This design results in enhanced internalization and delivery of the cytotoxin to cancer cells. In preclinical studies, ZW49 demonstrated complete tumor regressions in a panel of high and low HER2-expressing patient derived xenografts and promising efficacy in a model of breast cancer brain metastases. These results compared favorably when benchmarked against approved and leading HER2 ADCs in clinical development. Importantly, efficacy was observed at exposures that were well tolerated in preclinical studies suggesting a broad therapeutic window.

The poster is available through the conference website or through Zymeworks’ website at View Source

About the Azymetric Platform

The Azymetric platform enables the transformation of monospecific antibodies into bispecific antibodies, giving the antibodies the ability to simultaneously bind two different targets. This unique technology enables the development of multifunctional biotherapeutics that can block multiple signaling pathways, recruit immune cells to tumors, enhance receptor clustering degradation, and increase tumor-specific targeting. These features are intended to enhance efficacy while reducing toxicities and the potential for drug resistance. Azymetric bispecifics have been engineered to retain the desirable drug-like qualities of naturally occurring antibodies, including low immunogenicity, long half-life and high stability. In addition, they are compatible with standard manufacturing processes with high yields and purity, potentially significantly reducing drug development costs and timelines.

About the ZymeLink Platform

The ZymeLink platform is a modular suite of site-specific conjugation technologies, customizable linkers, and proprietary cytotoxic payloads designed for the targeted delivery of therapeutics with optimal tolerability and efficacy. The ZymeLink platform is compatible with traditional antibodies and with the Azymetric platform and is intended to facilitate the development of next-generation antibody-drug conjugates with broad therapeutic windows.

Novartis data demonstrates consistent efficacy and tolerability of Kisqali® combination therapy in HR+/HER2- advanced breast cancer in patients with difficult-to-treat visceral disease

On December 8, 2018 Novartis reported data from subgroup analyses of the three pivotal Phase III MONALEESA trials showing that Kisqali (ribociclib) plus endocrine therapy extended progression-free survival (PFS) compared to endocrine therapy alone, regardless of the presence of visceral metastases in pre-, peri- and postmenopausal women with hormone receptor positive, human epidermal growth factor receptor-2 negative (HR+/HER2-) advanced breast cancer1 (Press release, Novartis, DEC 8, 2018, View Source;advanced-breast-cancer-in-patients-with-difficult-to-treat-visceral-disease-300761974.html [SID1234531976]). These data will be presented today at the San Antonio Breast Cancer Symposium (SABCS) (Abstract #P6-18-07).

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"Nearly 60% of patients enrolled in the MONALEESA clinical trials had visceral metastases, and all benefited from treatment with ribociclib in combination with endocrine therapy," said Denise Yardley, MD, Principal Investigator, Sarah Cannon Research Institute. "These results, coupled with the NCCN and ABC4 recommended treatment guidelines for HR+ advanced breast cancer patients with visceral metastases, support the use of ribociclib combination therapy as a standard of care in this patient population."

In patients with visceral metastases, Kisqali plus endocrine therapy extended median PFS by 11.5 months in MONALEESA-2 (24.9 months vs 13.4 months) and 13.4 months in MONALEESA-7 (23.8 months vs 10.4 months) compared to endocrine therapy alone. Median PFS for patients with visceral metastases in the MONALEESA-3 trial still has not been reached compared to 16.5 months median PFS in patients receiving endocrine therapy alone1.

Kisqali plus endocrine therapy demonstrated consistent efficacy across the MONALEESA trials in patients with and without visceral metastases. In patients with visceral metastases and measurable disease, the overall response rate (ORR) in patients who received Kisqali plus endocrine therapy compared to endocrine therapy alone was 53% vs 40% (MONALEESA-2), 50% vs 38% (MONALEESA-7) and 48% vs 31% (MONALEESA-3). Patients without visceral disease showed an ORR of 59% vs 35%, 52% vs 32% and 49% vs 39% in the respective MONALEEA-2, MONALEESA-7 and MONALEESA-3 trials1.

"Patients living with HR+/HER2- advanced breast cancer who have visceral metastases often have a poorer prognosis and are at higher risk for treatment resistance and disease progression than those without," said Samit Hirawat, MD, Head, Novartis Oncology Global Drug Development. "These sub analyses reaffirm that it is critical to treat HR+ advanced breast cancer with a CDK4/6 combination therapy, such as Kisqali plus fulvestrant or an aromatase inhibitor, to give all patients, especially those with visceral metastases, the strongest option for delaying disease progression."

Adverse events for patients with visceral metastases were consistent with those observed in the overall study populations and generally manageable through dose interruptions or reductions1.

About Kisqali (ribociclib)
Kisqali (ribociclib) is the CDK4/6 inhibitor with the largest body of first-line clinical trial evidence demonstrating consistent, superior and sustained efficacy compared to endocrine therapy alone4.

Kisqali is a selective cyclin-dependent kinase inhibitor, a class of drugs that help slow the progression of cancer by inhibiting two proteins called cyclin-dependent kinase 4 and 6 (CDK4/6). These proteins, when over-activated, can enable cancer cells to grow and divide too quickly. Targeting CDK4/6 with enhanced precision may play a role in ensuring that cancer cells do not continue to replicate uncontrollably4.

Kisqali was initially approved by the US Food and Drug Administration (FDA) in March 2017 and by the European Commission in August 2017, as initial endocrine-based therapy for postmenopausal women with HR+/HER2- locally advanced or metastatic breast cancer in combination with an aromatase inhibitor based on findings from the pivotal MONALEESA-2 trial. In July 2018, Kisqali was approved by the FDA for the treatment of pre-, peri- or postmenopausal women in the US, and indicated for use in combination with fulvestrant as both first- or second-line therapy in postmenopausal women. In November 2018, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion recommending an expanded indication for Kisqali based on the MONALEESA-3 and MONALEESA-7 data. Regulatory filings are underway with other health authorities worldwide4.

Kisqali is approved for use in more than 70 countries around the world, including the United States and European Union member states. Kisqali is not currently approved for use in combination with fulvestrant or in premenopausal women in Europe. Kisqali was developed by the Novartis Institutes for BioMedical Research (NIBR) under a research collaboration with Astex Pharmaceuticals4.

Novartis is continuing to reimagine cancer by investigating Kisqali in early breast cancer (EBC). The NATALEE study is a Phase III clinical trial of Kisqali with endocrine therapy in the adjuvant treatment of HR+/HER2- EBC being conducted in collaboration with Translational Research In Oncology (TRIO)4.

About Novartis in Advanced Breast Cancer
For more than 30 years, Novartis has been tackling breast cancer with superior science, great collaboration and a passion for transforming patient care. With one of the most diverse breast cancer pipelines and one of the largest numbers of breast cancer compounds in development, Novartis leads the industry in discovery of new therapies and combinations, especially in HR+ advanced breast cancer, the most common form of the disease.

Kisqali (ribociclib) Important US Safety Information
KISQALI (ribociclib) is a prescription medicine used in combination with an aromatase inhibitor as the first hormonal-based therapy to treat pre/peri- and postmenopausal women and in combination with fulvestrant as the first hormonal-based therapy or following disease progression on hormonal therapy in postmenopausal women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer. It is not known if KISQALI is safe and effective in children. KISQALI can cause a heart problem known as QT prolongation. This condition can cause an abnormal heartbeat and may lead to death. KISQALI is not indicated for concomitant use with tamoxifen due to an increased risk of QT prolongation. Patients should tell their health care provider right away if they have a change in their heartbeat (a fast or irregular heartbeat), or if they feel dizzy or faint. KISQALI can cause serious liver problems. Patients should tell their health care provider right away if they get any of the following signs and symptoms of liver problems: yellowing of the skin or the whites of the eyes (jaundice), dark or brown (tea-colored) urine, feeling very tired, loss of appetite, pain on the upper right side of the stomach area (abdomen), and bleeding or bruising more easily than normal. Low white blood cell counts are very common when taking KISQALI and may result in infections that may be severe. Patients should tell their health care provider right away if they have signs and symptoms of low white blood cell counts or infections such as fever and chills. Before taking KISQALI, patients should tell their health care provider if they are pregnant, or plan to become pregnant as KISQALI can harm an unborn baby. Females who are able to become pregnant and who take KISQALI should use effective birth control during treatment and for at least 3 weeks after the last dose of KISQALI. Do not breastfeed during treatment with KISQALI and for at least 3 weeks after the last dose of KISQALI. Patients should tell their health care provider about all of the medicines they take, including prescription and over-the-counter medicines, vitamins, and herbal supplements since they may interact with KISQALI. Patients should avoid grapefruit or grapefruit juice while taking KISQALI. The most common side effects (incidence ≥20%) include white blood cell count decreases, nausea, infections, tiredness, diarrhea, vomiting, hair loss, headache, constipation, rash, and cough. The most common Grade 3/4 side effects (incidence >5%) were low neutrophils, low leukocytes, abnormal liver function tests, and low lymphocytes. Abnormalities were observed in hematology and clinical chemistry laboratory tests.

Update on the Phase III EAGLE trial of Imfinzi and tremelimumab in advanced head and neck cancer

On December 7, 2018 AstraZeneca and MedImmune, its global biologics research and development arm, reported overall survival (OS) results for the Phase III EAGLE trial. EAGLE is a randomised, open-label, multi-centre trial evaluating Imfinzi (durvalumab) monotherapy or Imfinzi in combination with tremelimumab, an anti-CTLA4 antibody, versus standard-of-care (SoC) chemotherapy in patients with recurrent or metastatic head and neck squamous cell carcinoma (HNSCC) who experienced disease progression following platinum-based chemotherapy, regardless of their PD-L1 tumour status (Press release, AstraZeneca, DEC 7, 2018, View Source [SID1234531946]).

Imfinzi monotherapy and the combination of Imfinzi plus tremelimumab did not meet the primary endpoints of improving OS compared to SoC chemotherapy in these hard-to-treat patients. The safety and tolerability profiles for Imfinzi and the combination with tremelimumab were consistent with previous experience.

Sean Bohen, Executive Vice President, Global Medicines Development and Chief Medical Officer, said: "The prognosis for recurrent or metastatic head and neck squamous cell cancer is very poor and new treatments for this group of cancers are urgently needed. While these results are disappointing, we remain committed to evaluating the potential of Imfinzi and other innovative medicines for patients with head and neck cancer. We look forward to seeing the results of the Phase III KESTREL trial of Imfinzi and tremelimumab in patients who have not received prior chemotherapy for recurrent or metastatic head and neck squamous cell carcinoma in the first half of 2019."

AstraZeneca will submit the results from the Phase III EAGLE trial for presentation at a forthcoming medical meeting.

About EAGLE
The EAGLE trial is a randomised, open-label, multi-centre, global, Phase III trial of Imfinzi (durvalumab) monotherapy or Imfinzi in combination with tremelimumab compared to standard-of-care chemotherapy in patients with recurrent or metastatic HNSCC who experienced progression following platinum-based chemotherapy, regardless of their PD-L1 tumour status.

The trial was conducted at 169 centres across 24 countries including the US, Europe, South America, Japan, Korea, Taiwan, Israel and Australia. The primary endpoint of the trial was OS, and secondary endpoints included progression-free survival, landmark OS, objective response rate and duration of response.

About HNSCC
Approximately 880,000 patients were diagnosed with head and neck cancer around the world in 2018. Two-thirds of patients diagnosed with head and neck cancer are in advanced stages (Stage III or IV), while the remaining one third are in the early stages of disease (Stage I or II). More than 90% of all head and neck cancers start in the squamous cells that line the mouth, nose and throat called head and neck squamous cell carcinomas (HNSCC).

About Imfinzi
Imfinzi (durvalumab) is a human monoclonal antibody that binds to PD-L1 and blocks the interaction of PD-L1 with PD-1 and CD80, countering the tumour’s immune-evading tactics and releasing the inhibition of immune responses.

Imfinzi is approved for unresectable, Stage III non-small cell lung cancer (NSCLC) in more than 40 countries including the US, EU, and Japan based on the Phase III PACIFIC trial. Imfinzi is also approved for previously-treated patients with advanced bladder cancer in the US, Canada, Brazil, Israel, India, United Arab Emirates, Australia and Hong Kong.

As part of a broad development programme, Imfinzi is also being tested as a monotherapy and in combination with tremelimumab, an anti-CTLA4 monoclonal antibody and potential new medicine, as a treatment for patients with NSCLC, small-cell lung cancer (SCLC), bladder cancer, head and neck cancer and other solid tumours.

About tremelimumab
Tremelimumab is a human monoclonal antibody and potential new medicine that targets the activity of cytotoxic T-lymphocyte-associated protein 4 (CTLA-4). Tremelimumab blocks the activity of CTLA-4, contributing to T-cell activation and boosting the immune response to cancer. Tremelimumab is being tested in a clinical trial programme in combination with Imfinzi in NSCLC, SCLC, bladder cancer, head and neck squamous cell carcinoma, liver cancer and blood cancers.

About AstraZeneca’s approach to immuno-oncology
IO is a therapeutic approach designed to stimulate the body’s immune system to attack tumours. At AstraZeneca and MedImmune, our biologics research and development arm, our IO portfolio is anchored by immunotherapies that have been designed to overcome anti-tumour immune suppression. We believe that IO-based therapies offer the potential for life-changing cancer treatments for the clear majority of patients.

We are pursuing a comprehensive clinical-trial programme that includes Imfinzi (anti-PDL1) as monotherapy and in combination with tremelimumab (anti-CTLA4) in multiple tumour types, stages of disease, and lines of therapy, using the PD-L1 biomarker as a decision-making tool to define the best potential treatment path for a patient. In addition, the ability to combine our IO portfolio with small, targeted molecules from across our Oncology pipeline, and from our research partners, may provide new treatment options across a broad range of tumours.

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MacroGenics Announces Partial Clinical Hold on MGD009 Phase 1 Studies

On December 7, 2018 MacroGenics, Inc. (NASDAQ: MGNX), a clinical-stage biopharmaceutical company focused on discovering and developing innovative monoclonal antibody-based therapeutics for the treatment of cancer, reported that on December 6, it received a letter from the U.S. Food and Drug Administration (FDA) indicating that a partial clinical hold has been placed on its Phase 1 monotherapy study of MGD009, a B7-H3 × CD3 bispecific DART molecule, as well as on a combination study of MGD009 and MGA012 (anti-PD-1) (Press release, MacroGenics, DEC 7, 2018, View Source [SID1234531963]). Under the partial clinical hold, no new patients will be enrolled in either study until the partial hold is lifted by the FDA. Current study participants may continue to receive drug at their pre-assigned dose.

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The partial clinical hold was initiated following MacroGenics’ reporting of hepatic adverse events on the MGD009 monotherapy trial to the FDA, including reversible elevations of transaminases with or without concurrent elevations of bilirubin. Although these events have been otherwise uncomplicated and short-lived in duration, MacroGenics also communicated to the FDA the company’s plans to amend the existing MGD009 studies with additional supportive care to mitigate these events. The FDA has placed the trials on partial clinical hold, pending review of additional details regarding these events, and satisfactory review of the planned amendments to the monotherapy and combination study protocols and related documents. MacroGenics will be working closely with the FDA to review these events and seek to resolve this clinical hold.

"MacroGenics’ top concern in conducting clinical trials is the safety of study participants," said Scott Koenig, M.D., Ph.D. "As we’ve identified to the FDA, we believe that transaminitis observed in patients administered MGD009 was likely a cytokine-mediated event. We are working with the FDA and will provide an update when we have additional information. This partial clinical hold does not impact ongoing clinical studies for enoblituzumab and MGC018, our other B7-H3-targeted molecules."
About MGD009
MGD009 is a humanized, bispecific DART molecule that recognizes both B7-H3 and CD3 and has a prolonged serum half-life. B7-H3 is a member of the B7 family of molecules involved in immune regulation and is over-expressed on a wide variety of cancer cells, including cancer stem cells, as well as on the supporting tumor vasculature and underlying tissues, or stroma. The intended mechanism of action of MGD009 is its ability to redirect T cells, via their CD3 component, to kill B7-H3-expressing cells.

In addition to MGD009, MacroGenics’ comprehensive B7-H3 franchise includes enoblituzumab, an Fc-optimized monoclonal antibody, as well as MGC018, an antibody-drug conjugate (ADC). These clinical molecules target B7-H3. MacroGenics retains worldwide rights to its franchise of three B7-H3-based molecules.

Amgen Announces 10 Percent Increase In 2019 First Quarter Dividend

On December 7, 2018 Amgen (NASDAQ:AMGN) reported that its Board of Directors declared a $1.45 per share dividend for the first quarter of 2019 (Press release, Amgen, DEC 7, 2018, View Source;p=RssLanding&cat=news&id=2379993 [SID1234531966]). The dividend will be paid on March 8, 2019, to all stockholders of record as of the close of business on Feb. 15, 2019. This represents a 10 percent increase from that paid in each of the previous four quarters.

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