ESSA Pharma Announces the Presentation of Additional Preclinical Data for EPI-7386 at the ESMO Virtual Congress 2020

On September 17, 2020 ESSA Pharma Inc. (Nasdaq: EPIX) (TSX-V: EPI), a clinical-stage pharmaceutical company focused on developing novel therapies for the treatment of prostate cancer, reported the presentation of data of ESSA’s clinical candidate, EPI-7386, at the ESMO (Free ESMO Whitepaper) Virtual Congress 2020 (Press release, ESSA, SEP 17, 2020, View Source [SID1234565320]).

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The oral poster presentation titled, "Preclinical profile of EPI-7386, a second-generation N-terminal domain androgen receptor inhibitor for the treatment of prostate cancer" was published on Thursday, September 17th.

The studies highlight new information about EPI-7386 including:

In vitro cellular gene expression analyses demonstrate that EPI-7386:
In an in vitro VCaP model, combination treatment of EPI-7386 with enzalutamide, apalutamide or darolutamide display broader and deeper inhibition of AR-associated transcriptional activity than higher doses of each single agent alone.
Shows superior activity to enzalutamide in an AR-V7-driven cellular model by modulating both AR-FL and AR-V7-driven gene expression with or without the addition of an external androgen such as R1881.
"Previously, we presented in vitro data demonstrating that combination treatment of EPI-7386 with enzalutamide displays broader and deeper inhibition of AR-associated transcriptional activity than higher doses of each single agent alone. These newest transcriptomic analyses demonstrate a similar effect on inhibiting AR-regulated genes by combining EPI-7386 with apalutamide and darolutamide. These data provide additional rationale for studying the potential benefit of combining EPI-7386 with a variety of second-generation anti-androgens in earlier line prostate cancer patients," said Dr. David R. Parkinson, President & Chief Executive Officer.

Positive Pivotal Data for Libtayo® (cemiplimab) Monotherapy in Locally Advanced Basal Cell Carcinoma Featured as a Late-breaking Presentation at ESMO

On September 17, 2020 Regeneron Pharmaceuticals, Inc. (NASDAQ: REGN) and Sanofi reported the presentation of positive results from the pivotal Phase 2 trial for the PD-1 inhibitor Libtayo (cemiplimab) in patients with locally advanced basal cell carcinoma (BCC) who had progressed on or were intolerant to hedgehog inhibitor (HHI) therapy (Press release, Regeneron, SEP 17, 2020, View Source [SID1234565318]). The data were shared in a late-breaking presentation at the European Society for Medical Oncology (ESMO) (Free ESMO Whitepaper) Virtual Congress 2020, and form the basis of regulatory submissions, including in the U.S. and European Union.

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"Advanced basal cell carcinoma can be an unrelenting, highly disfiguring disease, and there are no approved treatment options once a patient progresses on or becomes intolerant to hedgehog inhibitors," said Alexander Stratigos, M.D., Professor of Dermatology at the University of Athens Medical School at Andreas Sygros Hospital and a trial investigator. "This is the first time a prospective trial of an investigational medicine has shown a clinical benefit in this patient population, and the Libtayo data provide hope for this difficult-to-treat cancer."

Per independent central review, the objective response rate (ORR) was 31% among Libtayo-treated patients (n=84; 95% confidence interval [CI]: 21-42%), with a median follow-up of 15 months (range: 1-25 months). This included a 6% (n=5) complete and 25% (n=21) partial response rate. This is an increase from the ORR shared in May and includes two responses that were confirmed after the initial data analysis. Responses were seen regardless of baseline PD-L1 expression in tumor cells.

As of data cut-off, the median duration of response and median overall survival had not yet been reached. At one-year, 85% of responses were ongoing (95% CI; 61-95%), the probability of progression-free survival was 57% (95% CI: 44-67%), and the probability of overall survival was 92% (95% CI: 84-97%), according to Kaplan-Meier estimates.

No new Libtayo safety signals were observed. The most common treatment-related adverse events (AEs) were fatigue (25%, n=21), pruritus (14%, n=12) and asthenia (14%, n=12). Grade 3 or higher treatment-related AEs that occurred in at least 2 patients were colitis (5%, n=4), fatigue and adrenal insufficiency (2%, n=2 each). Fourteen patients (17%) discontinued treatment due to treatment-emergent AEs.

Libtayo was invented using Regeneron’s VelocImmune technology that utilizes a proprietary genetically-engineered mouse platform endowed with a genetically-humanized immune system to produce optimized fully-human antibodies. VelocImmune technology has been used to create multiple antibodies including Dupixent (dupilumab), Praluent (alirocumab) and Kevzara (sarilumab), which are approved in multiple countries around the world. Regeneron previously used these technologies to rapidly develop a treatment for Ebola virus infection, which is currently under review by the FDA, and to create REGN-COV2, a potentially preventative and therapeutic medicine for COVID-19.

Libtayo is being jointly developed by Regeneron and Sanofi under a global collaboration agreement. The use of Libtayo to treat advanced BCC is investigational and has not been fully evaluated by any regulatory authority.

About the Pivotal BCC Trial
In this ongoing, global Phase 2 trial, two cohorts of patients were studied: locally advanced BCC and metastatic BCC. All patients received Libtayo 350 mg intravenously every three weeks for up to 93 weeks or until disease progression. The primary endpoint is ORR, and key secondary endpoints include overall survival, progression free survival, duration of response, safety and tolerability. The median duration of response and median overall survival were estimated using Kaplan-Meier analyses. Detailed interim metastatic BCC data are planned for presentation at an upcoming medical meeting.

About BCC
BCC is a common type of non-melanoma skin cancer. While the vast majority of BCCs are caught early and easily cured with surgery and radiation, a small proportion of tumors can become advanced and penetrate deeper into surrounding tissues (locally advanced) or spread to other parts of the body (metastatic), which is more difficult to treat. In the U.S. alone, approximately 2 million new cases of BCC will be diagnosed every year, 20,000 U.S. patients will have advanced BCC and 3,000 patients will die of this disease.

About Libtayo
Libtayo is a fully-human monoclonal antibody targeting the immune checkpoint receptor PD-1 on T-cells. By binding to PD-1, Libtayo has been shown to block cancer cells from using the PD-1 pathway to suppress T-cell activation.

Libtayo is the first immunotherapy approved in the U.S., EU and other countries for adults with metastatic cutaneous squamous cell carcinoma (CSCC) or locally advanced CSCC who are not candidates for curative surgery or curative radiation. In the U.S., the generic name for Libtayo in its approved indication is cemiplimab-rwlc, with rwlc as the suffix designated in accordance with Nonproprietary Naming of Biological Products Guidance for Industry issued by the U.S. Food and Drug Administration. Outside of the U.S., the generic name for Libtayo in its approved indication is cemiplimab.

The extensive clinical program for Libtayo is focused on difficult-to-treat cancers. In skin cancer, this includes trials in adjuvant and neoadjuvant CSCC in addition to the pivotal trial in advanced BCC. Libtayo is also being investigated in pivotal trials in NSCLC and cervical cancer, as well as in trials combining Libtayo with either conventional or novel therapeutic approaches for both solid tumors and blood cancers. These potential uses are investigational, and their safety and efficacy have not been evaluated by any regulatory authority.

IMPORTANT SAFETY INFORMATION AND INDICATION FOR U.S. PATIENTS

What is Libtayo?
Libtayo is a prescription medicine used to treat people with a type of skin cancer called cutaneous squamous cell carcinoma (CSCC) that has spread or cannot be cured by surgery or radiation.

It is not known if Libtayo is safe and effective in children.

What is the most important information I should know about Libtayo?
Libtayo is a medicine that may treat a type of skin cancer by working with your immune system. Libtayo can cause your immune system to attack normal organs and tissues in any area of your body and can affect the way they work. These problems can sometimes become severe or life-threatening and can lead to death. You can have more than one problem at the same time. These problems may happen anytime during treatment or even after your treatment has ended.

Call or see your healthcare provider right away if you develop any symptoms of the following problems or these symptoms get worse:

Lung problems (pneumonitis). Signs and symptoms of pneumonitis may include new or worsening cough, shortness of breath, and chest pain.
Intestinal problems (colitis) that can lead to tears or holes in your intestine. Signs and symptoms of colitis may include diarrhea (loose stools) or more frequent bowel movements than usual; stools that are black, tarry, sticky or that have blood or mucus; and severe stomach-area (abdomen) pain or tenderness.
Liver problems (hepatitis). Signs and symptoms of hepatitis may include yellowing of your skin or the whites of your eyes, severe nausea or vomiting, pain on the right side of your stomach area (abdomen), drowsiness, dark urine (tea colored), bleeding or bruising more easily than normal, and feeling less hungry than usual.
Hormone gland problems (especially the adrenal glands, pituitary, thyroid and pancreas). Signs and symptoms that your hormone glands are not working properly may include headaches that will not go away or unusual headaches, rapid heartbeat, increased sweating, extreme tiredness, weight gain or weight loss, dizziness or fainting, feeling more hungry or thirsty than usual, hair loss, feeling cold, constipation, deeper voice, very low blood pressure, urinating more often than usual, nausea or vomiting, stomach-area (abdomen) pain, and changes in mood or behavior, such as decreased sex drive, irritability, or forgetfulness.
Kidney problems, including nephritis and kidney failure. Signs of these problems may include decrease in your amount of urine, blood in your urine, swelling in your ankles, and loss of appetite.
Skin problems. Signs of these problems may include rash, itching, skin blistering, and painful sores or ulcers in the mouth, nose, throat, or genital area.
Problems in other organs. Signs of these problems may include headache, tiredness or weakness, sleepiness, changes in heartbeat (such as beating fast, seeming to skip a beat, or a pounding sensation), confusion, fever, muscle weakness, balance problems, nausea, vomiting, stiff neck, memory problems, seizures (encephalitis), swollen lymph nodes, rash or tender lumps on skin, cough, shortness of breath, vision changes, or eye pain (sarcoidosis), seeing or hearing things that are not there (hallucinations), severe or persistent muscle pain, severe muscle weakness, low red blood cells (anemia), bruises on the skin or bleeding, and changes in eyesight.
Rejection of a transplanted organ. Your doctor should tell you what signs and symptoms you should report and monitor you, depending on the type of organ transplant that you have had.
Infusion (IV) reactions that can sometimes be severe and life-threatening. Signs of these problems may include chills or shaking, itching or rash, flushing, shortness of breath or wheezing, dizziness, fever, feeling of passing out, back or neck pain, and facial swelling.
Getting medical treatment right away may help keep these problems from becoming more serious.

Your healthcare provider will check you for these problems during your treatment with Libtayo. Your healthcare provider may treat you with corticosteroid or hormone replacement medicines. Your healthcare provider may delay or completely stop treatment if you have severe side effects.

Before you receive Libtayo, tell your healthcare provider about all your medical conditions, including if you:

have immune system problems such as Crohn’s disease, ulcerative colitis, or lupus;
have had an organ transplant;
have lung or breathing problems;
have liver or kidney problems;
have diabetes;
are pregnant or plan to become pregnant; Libtayo can harm your unborn baby
Females who are able to become pregnant:
Your healthcare provider will give you a pregnancy test before you start treatment.
You should use an effective method of birth control during your treatment and for at least 4 months after your last dose of Libtayo. Talk with your healthcare provider about birth control methods that you can use during this time.
Tell your healthcare provider right away if you become pregnant or think you may be pregnant during treatment with Libtayo.
are breastfeeding or plan to breastfeed. It is not known if Libtayo passes into your breast milk. Do not breastfeed during treatment and for at least 4 months after the last dose of Libtayo.
Tell your healthcare provider about all the medicines you take, including prescription and over- the-counter medicines, vitamins, and herbal supplements.

The most common side effects of Libtayo include tiredness, rash, diarrhea, muscle or bone pain, and nausea. These are not all the possible side effects of Libtayo. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088. You may also report side effects to Regeneron Pharmaceuticals and Sanofi at 1-877-542-8296.

Papyrus Therapeutics Inc. Signs Research Collaboration With Oxford Biomedica

On September 17, 2020 Papyrus Therapeutics, Inc. ("Papyrus" or the "Company"), an emerging biopharma company developing novel extracellular tumor suppressor therapies for the treatment of cancer and Oxford Biomedica plc (LSE:OXB or the "Group"), a leading gene and cell therapy group, reported the signing of a research collaboration agreement (Press release, Papyrus Therapeutics, SEP 17, 2020, View Source [SID1234565317]).

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"Bringing together Papyrus’ technology that targets cancer through tumor suppressor replacement and conditions the microenvironment to promote activation of CAR-T therapy simultaneously provides a potentially synergistic reprogramming of the tumor and its microenvironment to leverage CAR-T therapy."

The collaboration includes the assessment of the impact and therapeutic benefit of Papyrus’ PYTX-002, a potential first-in-class gene replacement therapy that will confer ‘cellular pharmacy’ properties on a CAR-T cell therapy developed by Oxford Biomedica, initially in preclinical in vivo models of solid tumors.

The Oxford Biomedica lentiviral platform technology was used in the first FDA and EMA approved CAR-T cell therapy – Kymriah (tisagenlecleucel). The Group’s lead CAR-T immunotherapy candidate, OXB-302, is a lentiviral CAR-T product targeting the 5T4 antigen expressed on the cell surface of many solid cancers.

"We are very pleased to have the opportunity to collaborate with Oxford Biomedica on the development on a CAR-T product candidate incorporating PYTX-002. This collaboration highlights the potential utility and versatility of the Company’s technology as a monotherapy as well as in combination with other treatment modalities as an effective cancer therapeutic in areas of high unmet medical need," said Co-Founder and Chief Executive Officer Dr. Paul Blake.

Papyrus Co-Founder and Chief Scientific Adviser Professor Hani Gabra said, "Bringing together Papyrus’ technology that targets cancer through tumor suppressor replacement and conditions the microenvironment to promote activation of CAR-T therapy simultaneously provides a potentially synergistic reprogramming of the tumor and its microenvironment to leverage CAR-T therapy."

Synthekine Launches with $82 Million Series A Financing to Advance Pipeline of Engineered Cytokine Therapeutics Optimized for Cancer and Autoimmune Diseases

On September 17, 2020 Synthekine Inc., an engineered cytokine therapeutics company, reported the closing of an $82 million Series A financing (Press release, Synthekine, SEP 17, 2020, View Source [SID1234565316]). The financing was co-led by Canaan Partners, Samsara BioCapital and The Column Group, with participation from other undisclosed investors. Synthekine was founded by K. Christopher Garcia, Ph.D., to leverage discoveries showing that cytokines can be tuned to enhance their therapeutic effects.

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Synthekine combines strengths in immunology, structural insights on cytokines and multiple engineering technologies to create optimized therapeutics against new and validated cytokine targets for the treatment of cancer and autoimmune disorders. Proceeds from this Series A financing will be used to advance Synthekine’s lead therapeutic programs into clinical studies, expand its discovery pipeline and hone its proprietary cytokine engineering platforms. The company currently has two lead programs in IND-enabling development: STK-012, an engineered Interleukin-2 (IL-2) partial agonist for the treatment of cancer, and the combination of STK-009 and SYNCAR-001, an orthogonal IL-2 ligand and a CD-19 CAR-T-cell therapy being studied in combination.

"Cytokines have a fundamental role in the immune system and represent an enormous opportunity for innovative therapeutics. However, most cytokines broadly activate a wide range of cells that can simultaneously stimulate and suppress the immune system, making drug development against these targets challenging," said Debanjan Ray, chief executive officer of Synthekine. "Chris Garcia has shown, for a wide range of therapeutically important cytokines, that cytokine efficacy and toxicity can be decoupled through structure-based protein engineering. These findings mean that many cytokines previously thought to be unsuitable as therapeutics can be transformed into safe and effective drugs. In addition to our highly differentiated IL-2-based programs, we have assembled multiple best-in-class technologies and an accomplished team to develop cytokine therapeutics by engineering them at the molecular level to enhance their activity and selectivity."

Unlocking cytokine therapeutics through unique structural biology insights

Cytokines are small, soluble proteins that are powerful regulators of the immune system and can stimulate a wide range of immune cells, primarily driven by their binding and interaction with cell surface receptors. Most cytokines are pleiotropic, meaning that a given cytokine can exert a range of responses across multiple cell types. Pleiotropy has proven to be a significant obstacle in the development of cytokine therapeutics. Existing cytokine therapeutics, such as aldesleukin (Proleukin) and interferons, demonstrate meaningful efficacy in cancer and other diseases but are limited by significant side effects.

Synthekine has licensed several cytokine programs and platforms from Stanford University. Research conducted in the Garcia lab at Stanford led to insights into the interaction of cytokines and their receptors, allowing researchers to engineer modified cytokines to deliver selective activity to particular cell types of therapeutic interest, giving them the potential for optimized efficacy, a larger therapeutic window and improved safety for patients. This research has been responsible for determining the three-dimensional structures for many different cytokine/receptor complexes, including IL-1, IL-2, IL-4, IL-6, IL-13, IL-15, IL-17, IL-23 and the three different classes of interferons.

A deep preclinical pipeline and proprietary platform

Synthekine is advancing several preclinical programs and innovative platform technologies. These include:

STK-012 – Partial Agonist of IL-2: Designed to selectively agonize T cells that recognize tumor antigens, Synthekine’s lead immuno-oncology IL-2 partial agonist STK-012 has demonstrated single-agent activity in preclinical tumor models. The company anticipates filing an IND in 2021 for this potent immunotherapy.
STK-009 – Orthogonal IL-2 System: Designed to selectively activate CAR-Ts and other adoptive cell therapies (ACTs) in vivo to improve efficacy, persistence and durability of CAR-Ts and other ACTs. Data evaluating STK-009, an orthogonal IL-2 ligand, with SYNCAR-001, an orthogonal IL-2 receptor-modified CD-19 targeted CAR-T, were presented at the American Association for Cancer Research (AACR) (Free AACR Whitepaper) Virtual Annual Meeting in 2020 and showed the ability to selectively harness the potent anti-tumoral T-cell effector functions of IL-2 and improve the efficacy, durability and manufacturability of CAR-T cell therapy. Synthekine anticipates filing an IND in 2021 for the STK-009/SYNCAR-001 combination.
Synthekine platform: Designed as a combinatorial engineering platform, synthekines are surrogate cytokine agonists that can combine cytokine receptors and drive new signaling activities without reliance on the wild type cytokine. The company is developing synthekines across several families of cytokines receptors.
A collaborative company formation effort and seasoned leadership team

The founding members of Synthekine’s board of directors include Tim Kutzkey, Ph.D., managing partner of The Column Group; Srinivas Akkaraju, Ph.D., founding partner of Samsara BioCapital; and Julie Grant, general partner at Canaan Partners. Synthekine has also appointed biopharma veteran Nils Lonberg as an independent member of its board of directors.

Synthekine’s executive team is led by Debanjan Ray as chief executive officer. Mr. Ray was previously chief financial officer and head of business development at CytomX Therapeutics, where he was responsible for leading financing efforts and securing multiple strategic collaborations with major pharmaceutical companies that generated more than $400 million in upfront payments and up to $4 billion in milestones. The executive team also includes Martin Oft, M.D., as chief development officer, Rob Kastelein, Ph.D., as head of therapeutic discovery and Gregory Yedinak as senior vice president of technical operations.

Synthekine’s scientific advisory board is led by its founder, K. Christopher Garcia, Ph.D., professor of molecular and cellular physiology and structural biology at Stanford University School of Medicine, a Howard Hughes Medical Institute (HHMI) investigator and a member of both the National Academy of Sciences and the National Academy of Medicine.

BeiGene Presents Data at ESMO Virtual Congress 2020 on Phase 3 Trial of Tislelizumab in First-Line Non-Squamous Non-Small Cell Lung Cancer and Phase 2 Trial of Pamiparib in Advanced Ovarian Cancer

On September 17, 2020 BeiGene, Ltd. (NASDAQ: BGNE; HKEX: 06160), a commercial-stage biotechnology company focused on developing and commercializing innovative medicines worldwide, reported the first reported data from RATIONALE 304, the Phase 3 trial of its anti-PD-1 antibody tislelizumab in combination with chemotherapy as a potential first-line treatment for patients with locally advanced or metastatic non-squamous non-small cell lung cancer (NSCLC), and the first reported data from the pivotal Phase 2 trial of its investigational PARP inhibitor pamiparib in advanced ovarian cancer (OC) at the European Society for Medical Oncology (ESMO) (Free ESMO Whitepaper) Virtual Congress 2020, which takes place on September 19-21 (Press release, BeiGene, SEP 17, 2020, View Source [SID1234565315]).

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"We are pleased to share the promising RATIONALE 304 results, which were used to support our recently accepted supplemental new drug application in first-line non-squamous NSCLC in China," commented Yong (Ben) Ben, M.D., Chief Medical Officer, Immuno-Oncology at BeiGene. "BeiGene is evaluating tislelizumab in multiple Phase 3 trials for the treatment of lung cancer, including RATIONALE 307 in first-line squamous NSCLC, which was reported at ASCO (Free ASCO Whitepaper) 2020 and filed in China, RATIONALE 303 in second-line NSCLC, RATIONALE 315 in stage II/IIIA NSCLC, and RATIONALE 312 in first-line extensive-stage small cell lung cancer. Our hope is to advance our broad tislelizumab development program in lung cancer to potentially improve treatment outcomes for the most prevalent cancer, both globally and in China."

"In addition to our Phase 3 data on tislelizumab, we are glad to report that the pivotal Phase 2 data of pamiparib in advanced ovarian cancer patients with BRCA1/2 mutations demonstrated high objective response rates in both platinum-sensitive and platinum-resistant subtypes, and we look forward to advancing pamiparib, which is currently under regulatory review in China," added Dr. Ben.

RATIONALE 304, Phase 3 Trial of Tislelizumab in Combination with Chemotherapy in First-Line Locally Advanced or Metastatic Non-Squamous NSCLC

Poster #1263P

"Tislelizumab in combination with pemetrexed and platinum chemotherapy has demonstrated encouraging results among advanced NSCLC patients with non-squamous histology, including a median progression-free survival of 9.7 months and an overall response rate of 57.4 percent. We are hopeful that tislelizumab can bring a new treatment option to patients with lung cancers in China," commented Shun Lu, M.D., Ph.D., Professor of Shanghai Chest Hospital at Jiao Tong University and lead investigator for the trial.

RATIONALE 304 is a randomized, open-label, multi-center Phase 3 clinical trial of tislelizumab in combination with pemetrexed and platinum chemotherapy (either carboplatin or cisplatin) as a first-line treatment for patients with stage IIIB or stage IV non-squamous NSCLC, compared to pemetrexed and platinum alone (NCT03663205). A total of 334 patients in China were enrolled in the trial, randomized at 2:1 to receive tislelizumab (200 mg every three weeks) in combination with chemotherapy (Arm A) or chemotherapy alone (Arm B). As of the data cutoff on January 23, 2020, with a median follow-up time of 9.8 months, 97 patients (43.5%) remained on treatment in Arm A and 20 patients (18.0%) in Arm B. Results included:

The trial achieved the primary endpoint of progression-free survival (PFS) as assessed by independent review committee (IRC), with a median of 9.7 months in Arm A, a significant improvement compared to 7.6 months in the chemotherapy alone Arm B (p=0.0044; stratified hazard ratio [HR]=0.645 [95% CI: 0.462, 0.902]);
Higher objective response rate (ORR) and disease control rate (DCR) were achieved in patients who received tislelizumab in combination with chemotherapy as assessed by IRC per RECIST v1.1 – 57.4% (95% CI: 50.6, 64.0) and 89.2% (95% CI: 84.4, 93.0) in Arm A, compared to 36.9% (95% CI: 28.0, 46.6) and 81.1% (95% CI: 72.5, 87.9) in Arm B;
Longer duration of response (DoR) was observed in patients who received tislelizumab in combination with chemotherapy, with a median of 8.5 months (95% CI: 6.80, 10.58) in Arm A, compared to 6.0 months (95% CI: 4.99, not evaluable) in Arm B;
Treatment of tislelizumab in combination with platinum and pemetrexed was generally well-tolerated, with no new safety signals identified;
All patients in Arm A and 99.1% of patients in Arm B experienced at least one treatment-emergent adverse event (TEAE); TEAEs leading to permanent discontinuation of any component of treatment occurred in 25.7% and 9.1% of the patients in Arm A and Arm B, respectively;
Most treatment-related adverse events (TRAEs) were hematologic in nature and primarily mild-to-moderate in severity, as follows:
In Arm A, the most common (≥20.0%) Grade 1-2 TRAEs include anemia (68.0%), leukopenia (60.8%), thrombocytopenia (50.5%), nausea (42.3%), increased alanine aminotransferase (ALT; 41.4%), increased aspartate aminotransferase (AST; 38.7%), neutropenia (37.4%), fatigue (33.3%), decreased appetite (28.4%), and vomiting (24.8%);
In Arm B, the most common (≥20.0%) Grade 1-2 TRAEs include anemia (64.5%), leukopenia (59.1%), thrombocytopenia (50.0%), increased AST (44.5%), increased ALT (40.9%), nausea (39.1%), neutropenia (38.2%), fatigue (31.8%), decreased appetite (25.5%), and vomiting (20.9%);
Grade ≥3 TRAEs occurred in 67.6% of patients in Arm A and 53.6% in Arm B, with the most common (≥10.0%) in Arm A being neutropenia (44.6%), leukopenia (21.6%), thrombocytopenia (19.4%), and anemia (13.5%), and the most common (≥10.0%) in Arm B being neutropenia (35.5%), leukopenia (14.5%), thrombocytopenia (13.6%), and anemia (10.0%);
Immune-mediated AEs were reported in 57 patients in Arm A (25.7%), and most of them were mild-to-moderate in severity, with the most common ones being pneumonitis (9%), hypothyroidism (8.6%), and hyperthyroidism (2.7%); and
Across the trial, nine patients experienced a fatal TEAE, including seven in Arm A caused by pneumonitis (n=3), asphyxia, atrial fibrillation, cerebellar hemorrhage, and unspecified death (n=1, each), and two in Arm B caused by pneumonitis and embolism (n=1, each).
Pivotal Phase 2 Trial of Pamiparib in Advanced OC

Poster #820P

"Pamiparib demonstrated strong antitumor activity in patients with advanced ovarian cancer, having achieved clinically meaningful and durable responses in both platinum-sensitive and platinum-resistant patients with BRCA1/2 mutation. This is encouraging news for patients with relapsed disease or patients who discontinued standard treatment due to unacceptable toxicity, and we are excited about pamiparib’s potential to improve treatment outcomes for them," said Xiaohua Wu, M.D., Ph.D., Professor and Chair of Gynecologic Oncology Department at Fudan University Shanghai Cancer Center and lead investigator for the trial.

The preliminary results presented at ESMO (Free ESMO Whitepaper) 2020 were from a Phase 2 dose-expansion portion of a Phase 1/2 trial of pamiparib in patients with advanced ovarian cancer, fallopian cancer, and primary peritoneal cancer or advanced triple negative breast cancer (NCT03333915). A total of 113 patients in China with high-grade, non-mucinous, epithelial OC (including fallopian or primary peritoneal cancer), harboring germline BRCA1/2 mutation, following at least two prior lines of standard chemotherapy were enrolled in the pivotal Phase 2 portion of the trial, including 90 patients with advanced platinum-sensitive OC (PSOC) in Cohort 1, and 23 patients with advanced platinum-resistant OC (PROC) in Cohort 2. Patients received pamiparib 60 mg orally twice daily in 21-day cycles. The primary endpoint of the study is ORR as assessed by IRC per RECIST v1.1. As of the data cutoff on February 2, 2020, with a median follow-up time of 12.2 months (0.2, 21.5), results included:

In Cohort 1 of patients with PSOC:
ORR was 64.6% (95% CI: 53.3, 74.9), including eight complete responses (CRs) and 45 partial responses (PRs);
DCR was 95.1% (95% CI: 88.0, 98.7);
Cancer antigen (CA)-125 response rate was 79.7% (95% CI: 68.8, 88.2);
The median DoR was 14.5 months (95% CI: 11.1, not evaluable) and the median PFS was 15.2 months (95% CI: 10.35, not evaluable);
In Cohort 2 of patients with PROC:
ORR was 31.6% (95% CI: 12.6, 56.6), including six PRs;
DCR was 94.7% (95% CI: 74.0, 99.9);
CA-125 response rate was 38.1% (95% CI: 18.1, 61.6);
Pamiparib was generally tolerated, consistent in patients with PSOC and PROC, and similar to other PARP inhibitors;
Across the trial, the most common (≥20.0%) TEAEs of any grade included anemia (89.4%), nausea (68.1%), decreased neutrophil count (61.1%), decreased white blood cell count (60.2%), vomiting (50.4%), decreased platelet count (31.0%), decreased appetite (30.1%), asthenia (28.3%), diarrhea (22.1%), increased AST (21.2%), decreased lymphocyte count (21.2%), increased ALT (20.4%), and leukopenia (20.4%);
Across the trial, the most common (≥10.0%) Grade ≥3 TEAEs included anemia (41.6%), decreased neutrophil count (33.6%), decreased white blood cell count (19.5%), and leukopenia (10.6%); and
No myelodysplastic syndrome or significant complications potentially related to hematologic AEs, such as Grade ≥3 hemorrhage, fever, or infection, were reported in the trial.
To learn more about the data presented at the ESMO (Free ESMO Whitepaper) Virtual Congress 2020 and BeiGene’s clinical pipeline, visit our virtual booth at View Source

About Tislelizumab

Tislelizumab (BGB-A317) is a humanized IgG4 anti-PD-1 monoclonal antibody specifically designed to minimize binding to FcγR on macrophages. In pre-clinical studies, binding to FcγR on macrophages has been shown to compromise the anti-tumor activity of PD-1 antibodies through activation of antibody-dependent macrophage-mediated killing of T effector cells. Tislelizumab is the first drug from BeiGene’s immuno-oncology biologics program and is being developed internationally as a monotherapy and in combination with other therapies for the treatment of a broad array of both solid tumor and hematologic cancers.

Tislelizumab is approved by the China National Medical Products Administration (NMPA) as a treatment for patients with classical Hodgkin’s lymphoma who received at least two prior therapies and for patients with locally advanced or metastatic urothelial carcinoma with PD-L1 high expression whose disease progressed during or following platinum-containing chemotherapy or within 12 months of neoadjuvant or adjuvant treatment with platinum-containing chemotherapy.

In addition, three supplemental new drug applications for tislelizumab have been accepted by the Center for Drug Evaluation (CDE) of the NMPA and are under review, for first-line treatment of patients with advanced squamous non-small cell lung cancer (NSCLC) in combination with chemotherapy, for first-line treatment of patients with advanced non-squamous NSCLC in combination with chemotherapy, and for previously treated unresectable hepatocellular carcinoma.

Currently, 16 potentially registration-enabling clinical trials are being conducted in China and globally, including 12 Phase 3 trials and four pivotal Phase 2 trials.

Tislelizumab is not approved for use outside of China.

About Pamiparib

Pamiparib (BGB-290) is an investigational inhibitor of PARP1 and PARP2 which has demonstrated pharmacological properties such as brain penetration and PARP-DNA complex trapping in preclinical models. Discovered by BeiGene scientists, pamiparib is currently in global clinical development as a monotherapy or in combination with other agents for a variety of solid tumor malignancies. To date, more than 1,200 patients have been enrolled in clinical trials of pamiparib.

A New Drug Application (NDA) for pamiparib for patients with ovarian cancer has been accepted and granted priority review by CDE of the NMPA.