Overland ADCT BioPharma Announces First Patient Dosed in China with ZYNLONTA® in Pivotal Phase 2 Clinical Trial for Diffuse Large B-cell Lymphoma

On September 29, 2021 Overland ADCT BioPharma, a joint venture created by Overland Pharmaceuticals and ADC Therapeutics SA (NYSE: ADCT), reported the first patient has been dosed with ZYNLONTA in a pivotal Phase 2 clinical trial in patients with relapsed or refractory (r/r) diffuse large B-cell lymphoma (DLBCL) in China (Press release, Overland ADCT BioPharma, SEP 29, 2021, View Source [SID1234590478]). In April 2021, ZYNLONTA was granted accelerated approval by the U.S. Food and Drug Administration (FDA) as the first and only CD19-targeted antibody drug conjugate (ADC) as a single-agent treatment for adult patients with r/r DLBCL after two or more lines of systemic therapy. This local pivotal study mirrors ADC Therapeutics’ ongoing global pivotal Phase 2 clinical trial of ZYNLONTA and its results are intended to support the potential registration of ZYNLONTA in China.

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"After receiving early FDA approval of ZYNLONTA in April, we are pleased that our colleagues at Overland ADCT BioPharma have rapidly initiated a pivotal study to potentially benefit patients in China," said Chris Martin, PhD, Chief Executive Officer of ADC Therapeutics. "We are eager for this bridging study to be completed, and we hope that ZYNLONTA will ultimately be available to all patients who can benefit from it globally."

"Dosing the first patient in this pivotal trial is a key milestone for Overland ADCT BioPharma as we collaborate to expand the clinical reach of ZYNLONTA in greater China and Singapore," said Eric Koo, Chief Executive Officer of Overland ADCT BioPharma. "With many patients in China affected by r/r DLBCL, we remain committed to addressing this unmet medical need and delivering promising antibody drug conjugates for underserved patients around the world. Together with ADC Therapeutics, we look forward to the continued development and commercialization of ZYNLONTA in Asia."

ZYNLONTA, Overland ADCT BioPharma’s lead product candidate, is an ADC composed of a humanized monoclonal antibody directed against human CD19 and conjugated to a pyrrolobenzodiazepine (PBD) dimer cytotoxin. In clinical trials, ZYNLONTA has demonstrated significant single-agent clinical activity across a broad population of patients with r/r DLBCL, mantle cell, and follicular lymphomas.

The China Phase 2, multi-center, open-label, single-arm study will evaluate the efficacy and safety of ZYNLONTA used as monotherapy in patients with r/r DLBCL.

About ZYNLONTA (loncastuximab tesirine-lpyl)

ZYNLONTA is a CD19-directed antibody drug conjugate (ADC). Once bound to a CD19-expressing cell, ZYNLONTA is internalized by the cell, where enzymes release a pyrrolobenzodiazepine (PBD) payload. The potent payload binds to DNA minor groove with little distortion, remaining less visible to DNA repair mechanisms. This ultimately results in cell cycle arrest and tumor cell death.

The U.S. Food and Drug Administration (FDA) has approved ZYNLONTA (loncastuximab tesirine-lpyl) for the treatment of adult patients with relapsed or refractory (r/r) large B-cell lymphoma after two or more lines of systemic therapy, including diffuse large B-cell lymphoma (DLBCL) not otherwise specified (NOS), DLBCL arising from low-grade lymphoma and also high-grade B-cell lymphoma. The trial included a broad spectrum of heavily pre-treated patients (median three prior lines of therapy) with difficult-to-treat disease, including patients who did not respond to first-line therapy, patients refractory to all prior lines of therapy, patients with double/triple hit genetics and patients who had stem cell transplant and CAR-T therapy prior to their treatment with ZYNLONTA. This indication is approved by the FDA under accelerated approval based on overall response rate and continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial.

ZYNLONTA is also being evaluated as a therapeutic option in combination studies in other B-cell malignancies and earlier lines of therapy.

Patent awarded for Concarlo-developed therapeutic to tackle treatment-resistant breast cancer

On September 29, 2021 Concarlo reported that US Patent 10,702,570 was issued by the United States Patent and Trademark Office (USPTO) for a metastatic breast cancer treatment (Press release, Concarlo Holdings, SEP 29, 2021, View Source [SID1234590526]). The patent, for which Concarlo is the exclusive licensee, covers IpY, a novel therapeutic peptide that addresses drug-resistant breast cancer by targeting a unique cellular pathway — p27Kip1. Concarlo has also announced that a new provisional patent application has been filed for modified versions of the therapeutic peptide that are believed to exhibit enhanced bioavailability. Concarlo is a Brooklyn-based biotechnology innovator dedicated to developing sophisticated, targeted therapies and diagnostics in the oncology space. The IpY technology is the first to address the high incidence of drug-refractory disease that develops with currently available CDK4 inhibitor (CDK4i) treatments. Such a solution has the potential to drastically increase overall survival of breast cancer patients.

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With more than 40,000 deaths due to metastatic breast cancer estimated for this year alone in the US, there is a pressing need to bring newer, more effective therapeutics to market. The recent introduction of CDK4i drugs, a class of medicines that directly targets the CDK4/6 pathway implicated in many malignancies, has had a significant impact on the way in which the disease is managed. However, such therapeutics are associated with patients transitioning to a treatment-resistant form of the condition, despite initial extended periods of remission. Backed by more than 20 years of research and development expertise, Concarlo has developed IpY and a companion diagnostic, ApY, to effectively overcome the issue of CDK4i resistance and roll out a more targeted treatment approach for optimized patient outcomes.

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"Despite the clinical efficacy of CDK4 inhibitors, we’re seeing that primary or secondary resistance to therapy is presenting a significant challenge to overall survival," commented Dr. Dominique Bridon, Chief Development Officer at Concarlo. "With the IpY technology and its unique mechanism of action, we’re effectively targeting CDK4 while simultaneously inhibiting another target — CDK2 — which has been found to be a key molecular player in the development of drug resistance. In doing so, we are the first company to successfully address the CDK4i resistance issue to provide long-term durable tumor arrest. Combined with its highly specific targeting and low toxicity profile, the positive impact of this drug on the breast cancer treatment landscape is hard to understate."

HUTCHMED Highlights Oral Presentations at 2021 Chinese Society of Clinical Oncology Annual Meeting

On September 29, 2021 HUTCHMED (China) Limited ("HUTCHMED") (Nasdaq/AIM: HCM, HKEX: 13) reported that new and updated clinical data from several ongoing combination studies of surufatinib (SULANDA in China) or fruquintinib (ELUNATE in China) with PD-1 inhibitors were presented at the 24th Chinese Society of Clinical Oncology (CSCO) Annual Meeting which has been taking place on September 25-29, 2021 (Press release, Hutchison China MediTech, SEP 29, 2021, View Source [SID1234590547]).

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SURUFATINIB
Title: A phase II study of surufatinib in combination with toripalimab in patients with advanced neuroendocrine carcinoma: an updated analysis
Lead Author Lin Shen, MD, Peking University Cancer Hospital & Institute
Type: Oral presentation
Session Number: CSCO Innovation Presentation 1-Session 2-#13

Patients with advanced neuroendocrine carcinoma ("NEC") have a poor prognosis and limited treatment options after first-line treatment. 5-year survival rates are low.[i] Surufatinib is approved for the treatment of patients with advanced or metastatic pancreatic and extra-pancreatic neuroendocrine tumors in China. Toripalimab is a monoclonal humanized IgG4 PD-1 antibody that previously demonstrated antitumor activity and safety in treating recurrent or metastatic neuroendocrine neoplasms ("NENs").[ii] Results from a Phase II study of the combination of surufatinib with toripalimab was first presented at the 2021 American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper) Annual Meeting (ASCO 2021).[iii]

In this updated analysis, at later data cutoff date of July 30, 2021, all 21 enrolled patients were efficacy evaluable, with average duration of treatment of 4.9 months (range 1-19). Median overall survival ("OS"), reported for the first time, was 10.3 months (95% CI: 9.1-not reached). The median progression-free survival ("PFS") was 4.14 months (95% CI: 1.5-5.5) and median duration of response ("DoR") was 4.1 months (95% CI: 3.0-not reached). The confirmed objective response rate ("ORR") was 23.8% (95% CI: 8.2-47.2) and disease control rate ("DCR") was 71.4% (95% CI: 47.8-88.7).

All patients experienced treatment-related adverse events ("TRAEs"), including 9 (42.9%) who experienced grade 3 or above TRAEs. 1 (4.8%) patient reported treatment-related serious adverse events ("SAEs"). Hyperglycemia (3 [14.3%]), hypertension (2 [9.5%]) and hypertriglyceridemia (2 [9.5%]) were the most commonly (more than one patient) reported grade 3 or above TRAEs. There were no TRAEs that led to treatment discontinuation or treatment-related deaths.

This updated analysis demonstrated the rationale of surufatinib plus toripalimab in the second-line setting for the treatment of patients with advanced NEC. A randomized phase III study SURTORI-01 has been initiated to further confirm the efficacy and safety of this combination therapy.

FRUQUINTINIB
Title: Fruquintinib plus sintilimab in patients with advanced endometrial cancer: a multicentre, open-label, single-arm, phase II clinical trial
Lead Author Xiaohua Wu, MD, Fudan University Shanghai Cancer Center
Type: Oral presentation
Session Number: CSCO Innovation Presentation 2-Session 2-#9

Platinum-based systemic chemotherapy is the standard first-line treatment for advanced endometrial cancer ("EMC"). However, patients who progress following first-line chemotherapy have limited treatment options, and the prognosis remains poor. Therefore, an important unmet medical need remains in patients with advanced EMC. Chemotherapy ORR is approximately 16%, while anti-angiogenesis inhibitors and/or immune checkpoint inhibitors have demonstrated less than a 15% ORR, with the exception of EMC patients with high microsatellite instability or mismatch repair defects (about 16% of EMC patients).[iv] Fruquintinib is a highly selective vascular endothelial growth factor receptor ("VEGFR") inhibitor and sintilimab is an anti-PD-1 monoclonal antibody. This Phase II study aims to assess the efficacy and safety of fruquintinib in combination with sintilimab for advanced EMC.

As of data cutoff date of August 31, 2021, 35 patients were enrolled, including 7 treatment-naïve and 28 pretreated patients. Of them, 29 were efficacy evaluable, 4 were treatment-naïve and 25 were pretreated. All 4 treatment-naïve patients experienced confirmed tumor response, for ORR of 100% (95% CI: 39.8-100.0), and median PFS was not reached. Among the 25 pretreated patients, the confirmed ORR was 32.0% (95% CI: 14.9-53.5), DCR was 92.0% (95% CI: 74.0-99.0) and the median PFS was 6.9 months (95% CI: 4.1-NR). Among the 19 proficient mismatch repair (pMMR) patients in pretreated cohort, the confirmed ORR was 36.8% (95% CI: 16.3-61.6), DCR was 94.7% (95% CI: 74.0-99.9), median PFS was 6.9 months (95% CI: 4.1-NR), and the median OS was not reached.

Among the 35 enrolled patients, 33 (94.3%) patients experienced TRAEs, including 17 (48.6%) who experienced grade 3 or above TRAEs. TRAEs of grade 3 or above that occurred in more than 10% of patients were hypertension (4 [11.4%]) and proteinuria (4 [11.4%]). 5 (14.3%) patients reported treatment-related SAEs. 2 patients experienced TRAEs that led to discontinuation of sintilimab while 1 patient each discontinued fruquinintinb alone or the fruquintinib and sintilimab combination.

Regulatory discussions for this combination in China are currently under discussions with regulators, which may lead to the initiation of a pivotal study before year end.

Title: A phase II study of fruquintinib plus sintilimab in pretreated patients with advanced hepatocellular carcinoma
Lead Author Shukui Qin, MD, Eastern Theater General Hospital, Qinhuai Medical Area
Type: Oral presentation
Session Number: CSCO Innovation Presentation 2-Session 1-#7

Patients with hepatocellular carcinoma ("HCC"), the most common type of liver cancer, have very limited treatment options. Combination use of VEGF targeting therapy with immunotherapy has demonstrated remarkable clinical benefits in first-line HCC, but its anti-tumor activity in second- or later line treatments is not established. This phase II study was performed to assess the combination of fruquintinib, a highly selective VEGFR inhibitor, with sintilimab, an anti-PD-1 antibody, in patients with advanced HCC who were treated with at least one prior line of treatment, including either sorafenib or lenvatinib. The combination demonstrated preliminary anti-tumor efficacy and durability in these patients.

As of data cutoff date of August 31, 2021, among 19 response-evaluable patients, the confirmed ORR was 31.6% (95% CI: 12.6-56.6), and the DCR was 89.5% (95% CI: 66.9-98.7). The median DoR was not reached. The median PFS was 6.9 months (95% CI: 4.1-not reached). With a median follow up of 7.4 months, the median OS was not reached.

Among 21 enrolled patients, 20 (95.2%) patients experienced TRAEs, including 7 (33.3%) who experienced grade 3 or above TRAEs. No TRAEs of grade 3 or above occurred in more than one patient. 4 (19.0%) patients reported treatment-related SAEs. TRAEs leading to fruquintinib discontinuation and sintilimab discontinuation were reported in 2 (9.5%) and 1 (4.8%) patient, respectively.

Registration plans for this combination regimen in China are currently under discussions with investigators.

Title: Fruquintinib plus sintilimab in patients with advanced renal cell carcinoma: results from a phase II clinical trial
Lead Author Dingwei Ye, MD, Fudan University Shanghai Cancer Center
Type: Oral presentation
Session Number: CSCO Innovation Presentation 2-Session 2-#13

In first-line clear-cell renal cell carcinoma ("ccRCC"), clinical benefits have been demonstrated for the combination of antiangiogenic therapy and immunotherapy. However, there is limited evidence on the benefits of this combination in the second-line setting. This phase II study aimed to evaluate the efficacy and safety of fruquintinib plus sintilimab in second-line treatment of ccRCC, which has shown encouraging anti-tumor efficacy and durability in these patients.

As of data cutoff date of August 31, 2021, all 20 enrolled patients were efficacy evaluable. 19 patients previously received VEGFR inhibitors, and 2 received interferon. The confirmed ORR was 55.0% (95% CI: 31.5-76.9) and DCR was 85.0% (95% CI: 62.1-96.8). The median PFS was not reached with a median follow up of 8.2 months. PFS rate at 9 months was 63.6% (95% CI: 38.1-80.9). Median treatment time was 38.6 weeks, with the longest being over 50 weeks and ongoing.

All patients experienced TRAEs, including 9 (45%) who experienced grade 3 or above TRAEs. The most common (more than one patient) grade 3 or above TRAEs were increased amylase (3 [15.0%]), hypertriglyceridemia (3 [15.0%]), hypertension (2 [10.0%]) and lipase increased (2 [10.0%]). Treatment-related SAEs were reported in 2 patients (10.0%). There were no TRAEs that led to treatment discontinuation.

Registration plans for this combination regimen in China are currently under discussions with investigators.

About Surufatinib (SULANDA in China)
Surufatinib is a novel, oral angio-immuno kinase inhibitor that selectively inhibits the tyrosine kinase activity associated with VEGFR and FGFR, which both inhibit angiogenesis, and CSF-1R, which regulates tumor-associated macrophages, promoting the body’s immune response against tumor cells. Its unique dual mechanism of action may be very suitable for possible combinations with other immunotherapies, where there may be synergistic anti-tumor effects.

HUTCHMED currently retains all rights to surufatinib worldwide.

About Fruquintinib (ELUNATE in China)
Fruquintinib is a highly selective and potent oral inhibitor of VEGFRs -1, -2 and -3. VEGFR inhibitors play a pivotal role in blocking tumor angiogenesis. Fruquintinib was designed to improve kinase selectivity to minimize off-target toxicities, improve tolerability and provide more consistent target coverage. The generally good tolerability in patients to date, along with fruquintinib’s low potential for drug-drug interaction based on preclinical assessment, suggests that it may also be highly suitable for combinations with other anti-cancer therapies.

HUTCHMED retains all rights to fruquintinib outside of China. In China, HUTCHMED is partnered with Eli Lilly and Company and is responsible for development and execution of all on-the-ground medical detailing, promotion and local and regional marketing.

Collaboration with Sponsor 丨 Bebetter Med HDAC/PI3K Dual-target Inhibitor BEBT-908 Proposed for Inclusion in Breakthrough Therapy List

On September 29, 2021 BeBetter Medicine reported that according to the CDE website, Bebetter Med’ HDAC/PI3K dual-target inhibitor BEBT-908 is proposed for inclusion in the breakthrough therapy list for the third-line treatment of relapsed or refractory diffuse large B-cell lymphoma (r/r DLBCL) (Press release, BeBetter Medicine Technology, SEP 29, 2021, View Source [SID1234633497]).

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BEBT-908 is Bebetter Med’s first HDAC/PI3K dual target inhibitor proposed for inclusion in the breakthrough therapy list Panacro, entrusted by Bebetter Med, has engaged in CRO services such as medical R&D strategy development, medical monitoring, data management and statistical analysis since September 25, 201

The technical team of Panacro responded quickly and solve the problems encountered in the clinical trials in a professional and efficient manner. In the NDA of breakthrough therapy, the medical division, data division and statistical division worked together to achieve a good presentation of the Phase IIa statistical analysis report and clinical study report in a short period of time, which was highly recognized by the sponsor and CDE.

"Currently, five clinical studies have been initiated with BEBT-908, among which, Phase II clinical studies targeting a variety of hematologic tumors such as follicular lymphoma, chronic lymphocytic leukemia/small lymphocytic lymphoma, Walden’s macroglobulinemia, marginal zone lymphoma, and peripheral T-cell lymphoma have been initiated, and solid tumor indications are also under clinical exploration, and Panacro is honored to participate,"said Du Xiaojian, Chief Medical Officer of Panacro.

In the future, Panacro, by leveraging its professional technical ability and quality service, will make persistent efforts to promote local innovative drugs to benefit the majority of patients as soon as possible!"

Syros Announces First Patient in Dose Confirmation Study of SY-2101, a Novel Oral Form of Arsenic Trioxide, in Acute Promyelocytic Leukemia

On September 29, 2021 Syros Pharmaceuticals (NASDAQ:SYRS), a leader in the development of medicines that control the expression of genes, reported that the first patient has been dosed in the dose confirmation study of SY-2101, a novel oral form of arsenic trioxide (ATO) (Press release, Syros Pharmaceuticals, SEP 29, 2021, View Source [SID1234590480]). The trial will evaluate the pharmacokinetics (PK), safety, and tolerability of SY-2101 to confirm the optimal dose to advance into a planned Phase 3 clinical trial in newly diagnosed acute promyelocytic leukemia (APL) patients.

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"The current standard of care cures most patients but is tremendously burdensome, requiring regular and lengthy infusions of an IV formulation of ATO over nearly a yearlong course of treatment," said Farhad Ravandi, M.D., Professor of Medicine, Chief of Section of Acute Myeloid Leukemia, Department of Leukemia at The University of Texas – MD Anderson Cancer Center. "An oral form of ATO that offers similar efficacy while dramatically reducing the treatment burden would represent a major advance for APL patients. The preliminary Phase 1 data for SY-2101 are very promising, and I look forward to its continued advancement in the current and future studies."

APL is a well-defined subtype of acute myeloid leukemia (AML), which accounts for about 10% of AML cases, with approximately 2,000 APL patients diagnosed annually in the United States and Europe. An intravenously administered formulation of ATO is approved for use in combination with All-Trans-Retinoic-Acid (ATRA) in newly diagnosed APL and, while curative in more than 80% of patients, its administration requires up to 140 infusions over the typical 10-month course of induction and consolidation treatment. In an earlier Phase 1 clinical trial, SY-2101, which is dosed once daily, demonstrated oral bioavailability, PK exposures similar to IV ATO, and a generally well-tolerated safety profile.

"We are thrilled to now be dosing patients in our dose confirmation study of SY-2101," said David A. Roth, M.D., Chief Medical Officer at Syros. "This milestone represents an important step toward delivering a new option for people with APL and a meaningful advance in our efforts to build a leading portfolio of targeted hematology therapies. We believe SY-2101 could quickly become the new standard of care for APL by offering patients similar efficacy with a substantially more accessible and convenient therapy. We plan to move swiftly from our dose confirmation study into a Phase 3 trial next year, with the goal of filing a New Drug Application (NDA) in 2024."

The dose confirmation study is expected to enroll up to 24 patients with newly diagnosed APL and will evaluate safety, tolerability, and PK as well as the effect of food on the absorption of SY-2101. Patients will be enrolled during the consolidation phase of their APL treatment and will receive single doses of SY-2101 in a fasted state, SY-2101 in a fed state, and IV ATO. Patients will then have the option to roll over into a multiple-dose cohort to receive either SY-2101 or IV ATO, which will provide additional data on the steady state PK and safety of SY-2101 in comparison to IV ATO. Syros expects to report data from this study in the first half of 2022.

Based on the results of the dose confirmation study, Syros expects to initiate a Phase 3 clinical trial in newly diagnosed APL patients. Based on input from the FDA, Syros believes molecular complete response rate and event-free survival in comparison to historical control data with IV ATO may support accelerated and full approval, respectively.