On June 4, 2021 Cullinan Oncology, Inc. (Nasdaq: CGEM) ("Cullinan"), an oncology company seeking to drive shareholder returns by focusing on the patient, reported additional details pertaining to Cullinan Pearl’s ongoing Phase 1/2a trial of CLN-081 in Non-Small Cell Lung Cancer (NSCLC) patients whose tumors harbor epidermal growth factor receptor (EGFR) exon 20 insertion mutations (Press release, Cullinan Oncology, JUN 4, 2021, View Source [SID1234583537]). CLN-081 is an orally available, irreversible EGFR inhibitor, utilizing a unique pyrrolopyrimidine scaffold that was designed to selectively target cells expressing mutant EGFR variants, including exon 20, while sparing cells expressing wild type (WT) EGFR.

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

These data will be featured in an on-demand poster presentation available this morning at 9:00 am EDT at the 2021 American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper) Annual Meeting and during a company sponsored webinar at 10:30 am EDT today, which can be accessed here or in the ‘Events’ section on Cullinan’s investor website.

"We remain encouraged with CLN-081’s emerging profile," stated Owen Hughes, Cullinan’s Chief Executive Officer. "In heavily pretreated patients, CLN-081 continues to show antitumor activity across the dose range, with a safety profile that appears to be differentiated, most specifically with respect to GI adverse events."

The current analysis of the ongoing trial evaluated a total of 45 NSCLC patients with EGFR exon 20 insertion mutations who received at least one dose of CLN-081 as of the April 1, 2021, data cutoff, and were evaluable for safety. CLN-081 was dosed orally, at dose levels including 30, 45, 65, 100 and 150 mg twice daily (BID). As of the data cutoff, 42 of 45 patients were response evaluable across all dose cohorts tested.

Overall Safety:

Regarding treatment related adverse events (TRAEs) associated with WT EGFR inhibition:

Rash has been limited to Grade 1 and 2 events (76% of patients experienced an event across all doses as of the data cutoff); events were manageable with conventional supportive care; no patients have experienced Grade ≥3 TRAE rash.

Similarly, diarrhea has been mostly limited to Grade 1 and 2 events (22% across the dose range) as of the data cutoff, with a single Grade ≥3 TRAE at the highest dose tested to date, 150 mg BID, which resolved with supportive care. No prophylactic regimen has been required to ameliorate the incidence or severity of diarrhea to date.
Overall Efficacy:

Objective partial responses (PR) were observed in 21 of 42 (50%) response evaluable patients treated across all dose levels.

Of the 21 PRs as of the data cutoff, 13 were confirmed (31% confirmed objective response rate), 5 were pending confirmation (i.e., patient had not reached their second post-baseline disease assessment as of the data cutoff), and 3 will remain unconfirmed.

41 of 42 (98%) response evaluable patients have achieved a best response of stable disease (SD) or PR, with 76% of all patients showing some degree of tumor regression at the initial scan post baseline (week 6).
100 mg BID Expansion Cohort:

In February 2021, Cullinan announced a Phase 2a expansion at the 100mg BID cohort, allowing enrollment of up to 36 patients.

Safety: Treatment-related rash has been limited to Grade 1 and 2 events (66%), manageable with conventional supportive care; no patients have experienced Grade ≥3 TRAE rash. In addition, the overall incidence of treatment-related diarrhea was 26%, with no Grade ≥3 events to date.

Efficacy: As of the data cutoff, objective responses were observed in 7 of 13 (54%) response evaluable patients; 6 of which were confirmed (46%) and 1 will remain unconfirmed.

Of the 13 response evaluable patients, 9 (69%) patients achieved disease control (PR of any duration or SD ≥ 6 months) as of the data cutoff; an additional 3 patients had stable disease and remained on treatment but had started therapy less than 6 months prior to data cutoff.
"We are pleased with the CLN-081 safety and efficacy data to date in our Phase 1/2a trial. CLN-081 has demonstrated antitumor activity in patients post systemic chemotherapy, including among patients who were also treated previously with other EGFR inhibitors and/or cancer immunotherapy, across the range of CLN-081 doses tested to date, and across a spectrum of exon-20 mutational sub-types," said Jon Wigginton, M.D., Chairman of the Cullinan Oncology Scientific Advisory Board and Senior Advisor. "We are working diligently to evaluate CLN-081 in additional patients, and to set the stage for further clinical advancement of CLN-081 in this group of patients with significant unmet need."

About CLN-081

CLN-081 is an orally available, irreversible EGFR inhibitor that was designed to selectively target cells expressing mutant EGFR variants, including Ins20, while sparing cells expressing wild type EGFR. In preclinical studies, CLN-081 demonstrated inhibition against traditional sensitizing mutations (exon 19 deletions and L858R), Ins20 (the third most common EGFR mutation), and other less common mutations (G719X, L861Q, and S768I).

Cullinan is evaluating various doses of CLN-081 in a Phase 1/2a trial in patients with NSCLC harboring Ins20 mutations that have progressed post chemotherapy. Based on pre-specified efficacy and safety criteria, Cullinan recently initiated Phase 2a dose expansion in the 100 mg BID dosing cohort, which will enable enrollment of up to 36 patients at this dose level, inclusive of 13 previously enrolled patients.

On June 4, 2021 Ocuphire Pharma, Inc. (Nasdaq: OCUP), a clinical-stage ophthalmic biopharmaceutical company focused on developing and commercializing therapies for the treatment of several eye disorders, reported it has entered into a securities purchase agreement with institutional investors for the purchase and sale of 3,076,923 shares of the Company’s common stock (the "Shares") and warrants to purchase 1,538,461 shares of the Company’s common stock (the "Warrants", and together with the Shares, the "Securities") at a combined purchase price of $4.875 per one Share and 0.5 Warrant in a registered direct offering priced at-the-market under Nasdaq rules (Press release, Rexahn, JUN 4, 2021, View Source [SID1234583554]). The Warrants will have an exercise price of $6.09 per share, will be exercisable on issuance date, and will expire five years following the issuance date. The closing of the offering is expected to occur on or about June 8, 2021, subject to the satisfaction of customary closing conditions.

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

A.G.P./Alliance Global Partners is acting as sole placement agent for the offering.

This offering is being made pursuant to an effective shelf registration statement on Form S-3 (File No. 333-252715) previously filed with the U.S. Securities and Exchange Commission (the "SEC"). A prospectus supplement describing the terms of the proposed offering will be filed with the SEC and will be available on the SEC’s website located at View Source Electronic copies of the prospectus supplement may be obtained, when available, from A.G.P./Alliance Global Partners, 590 Madison Avenue, 28th Floor, New York, NY 10022, or by telephone at (212) 624-2060, or by email at [email protected]. Before investing in this offering, interested parties should read in their entirety the prospectus supplement and the accompanying prospectus and the other documents that the Company has filed with the SEC that are incorporated by reference in such prospectus supplement and the accompanying prospectus, which provide more information about the Company and such offering.

This press release shall not constitute an offer to sell or the solicitation of an offer to buy nor shall there be any sale of these securities in any state or jurisdiction in which such offer, solicitation or sale would be unlawful prior to registration or qualification under the securities laws of any such state or jurisdiction.

On June 4, 2021 Y-mAbs Therapeutics, Inc. (the "Company" or "Y-mAbs") (Nasdaq: YMAB) a commercial-stage biopharmaceutical company focused on the development and commercialization of novel, antibody-based therapeutic products for the treatment of cancer, reported that Dr. Mark Souweidane, Memorial Sloan Kettering Cancer Center ("MSK") and Weill Cornell Medicine will present interim phase 1 dose-escalation data for omburtamab for diffuse intrinsic pontine glioma ("DIPG") at the American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper) ("ASCO") Virtual Annual Meeting on June 4, 2021 (Press release, Y-mAbs Therapeutics, JUN 4, 2021, View Source [SID1234583571])

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

The phase 1 dose-escalation study with administration via convection enhanced delivery ("CED"), showed that dosing of omburtamab radiolabeled with 8 mCi of 124-Iodine appeared to be well-tolerated and provided distribution volume to potentially cover tumor volumes of up to 20 cm3. The median overall survival of all 46 patients in the study increased by three to four months as compared to the historical control group. The study will continue dose escalation for both infused volume and dose.

"We are excited to share these results that significantly broaden the potential reach of omburtamab, which would be addressing a clear unmet medical need. The results pave the way for our multicenter phase 2 study in DIPG later this year, where we expect to give up to three repeated doses of omburtamab," stated Thomas Gad, founder, Chairman and President.

Dr. Claus Moller, Chief Executive Officer, continued, "We are expanding our omburtamab franchise significantly this year. While the iodine labeled omburtamab targets DIPG, CNS/LM from neuroblastoma and DSRCT, we have also initiated clinical trials for medulloblastoma and B7-H3 positive CNS metastasis with our lutetium labeled omburtamab."

Researchers at MSK developed omburtamab, which is exclusively licensed by MSK to Y-mAbs. As a result of this licensing arrangement, MSK has institutional financial interests in the product.

On June 4, 2021 Physicians from Dallas-based Texas Oncology and researchers from Seattle-based Navigating Cancer will present two posters highlighting the benefits of electronic patient management at the virtual 2021 ASCO (Free ASCO Whitepaper) Annual Meeting, which takes place June 4-8, 2021 (Press release, Navigating Cancer, JUN 4, 2021, View Source [SID1234583585]). The two poster presentations examine the impact that Navigating Cancer’s digital monitoring program, Health Tracker, has on symptom management for cancer patients at a large, multi-site community oncology practice.

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

The first poster session titled, "Implementation of Electronic Patient-Reported Outcomes (ePROs) for Symptom Monitoring in a Large Multi-Site Community Oncology Practice," is part one of the Texas Two-Step study, a two-part (hybrid) implementation-effectiveness evaluation of ePROs. In part one of the Texas Two-Step study, researchers found that utilization of the ePRO tool can help provide just-in-time symptom management and, despite the challenges of the global COVID-19 pandemic on cancer practices, implementation of ePROs for digital symptom monitoring across a large multi-site statewide cancer practice is feasible, and compliance is high. Step two of the Texas Two-Step study will evaluate the impact ePROs have on healthcare resource utilization, time on therapy, and symptom control.

"The data shows that digital healthcare systems like Health Tracker can help clinicians manage their patients’ symptoms quickly and efficiently, potentially leading to improved clinical outcomes, fewer visits to emergency departments, higher patient satisfaction, and compliance with therapy," said lead author Debra Patt, M.D., Ph.D., MBA, medical oncologist and executive vice president, public policy, and strategic initiatives at Texas Oncology. "For cancer patients especially, response time is critical, and this technology allows care teams to monitor a patient’s symptoms in real-time and swiftly respond to patients who are in need and require symptom control. It also gives us better insight on compliance with oral therapies."

The second poster session titled, "Improvement in Incident Resolution Time with the Implementation of an Electronic Patient Management Solution at a Community Oncology Practice," evaluates the impact of the digital monitoring program on time to symptom resolution – prolonged times to system resolution can lead to unnecessary emergency department visits. The researchers found that the program, with Plan Do Study Act (PDSA) cycles of quality improvement, can markedly improve incident resolution times, especially for symptom-related calls.

"Staying connected with cancer patients and monitoring their symptoms outside of the clinic can be challenging for busy clinicians," said Bill Bunker, CEO of Navigating Cancer. "This research demonstrates that when technology is effectively integrated into existing practice workflows, it can fill this care gap and drive improved outcomes and better experiences for patients."

Texas Oncology focuses on delivering quality cancer care and mitigating healthcare disparities for Texans fighting cancer through its locations in communities of all sizes throughout the state, including smaller cities and towns. In addition, telemedicine connects patients with care teams both locally and with access to specialized physician expertise in other cities. Online support groups, including nutrition support groups, serve patients no matter where they live so they can receive the critical support they need.

The full abstracts and both posters are available at NavigatingCancer.com/publications. Additional insights into the Texas Two-Step study are available in the JCO Clinical Cancer Informatics.

Abstract Summaries:

Implementation of Electronic Patient-Reported Outcomes for Symptom Monitoring in a Large Multi-Site Community Oncology Practice, Abstract 12103

Lead author: Debra Patt M.D., Ph.D., MBA, medical oncologist and executive vice president, public policy, and strategic initiatives at Texas Oncology

Patients initiating a new systemic therapy at one of 210 Texas Oncology practice sites were invited to use the Navigating Cancer ePRO platform from July-December 2020. Participating patients received a weekly prompt by SMS text message or email (patient choice) to self-report common symptoms and well-being via computer or smartphone. Severe self-reported symptoms triggered a real-time notification alert to a triage nurse to address the symptom.

Highlights:

More than 4,000 cancer patients initiating systemic therapy enrolled in the program throughout the study period with 25% of patients living more than 20 miles from their clinic.
Of the patients who were enrolled in the platform, 73% completed at least one ePRO assessment, and among these individuals, 65% of all available weekly ePRO assessments were completed.
SMS (89%) was strongly preferred over email (6%) or clinic collect (5%). SMS was also associated with the highest participation rate (77%) vs. email (54%) or clinic collect (45%).
Improvement in Incident Resolution Time with the Implementation of an Electronic Patient Management Solution at a Community Oncology Practice, Abstract 1578

Lead author: Lalan Wilfong, M.D., medical oncologist and executive vice president for value-based care and quality programs at Texas Oncology

Incident volumes and resolution times were monitored at all Texas Oncology locations along with the implementation of PDSA cycles, which had a goal of less than 90-minute resolution of symptom-related incidents. Utilizing Navigating Cancer’s electronic dashboard allowed Texas Oncology to continue this initiative during the pandemic as some staff could work remotely. Nurses could document if a potential emergency department visit was avoided, and these data points allowed the practice to establish comprehensive and strategic actions plans for quality improvement.

Highlights:

Resolution time for all incidents started at 3.2 hours pre-implementation and improved to 2.2 hours in December 2020.
Sixty-two percent of symptom-related incidents were resolved in less than one hour.
Eight percent of symptom-related incidents resulted in definite or probable emergency department avoidances by nursing assessment.
Shortness of breath, vomiting, chills, and weakness were the top symptom types addressed for emergency department avoidances.

On June 4, 2021 Shanghai Yingli Pharmaceuticals Ltd (Yingli Pharma), a clinical stage pharmaceutical company providing new therapies for cancer and metabolic diseases, reported that there will be three presentations on clinical trials sponsored by the company at the annual meeting of the American Society for Clinical Oncology (ASCO) (Free ASCO Whitepaper) June 4-7, 2021 (Press release, Yingli Pharmaceutical, JUN 4, 2021, View Source [SID1234583604]).

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

Linperlisib in Peripheral T cell lymphoma

The clinical trial report entitled "A phase Ib study of a PI3Kδ inhibitor Linperlisib in patients with relapsed or refractory peripheral T-cell lymphoma" was presented at the June 4, 2021 proceedings of the conference.

In this phase Ib study that enrolled 38 relapsed and refractory Peripheral T cell lymphoma patients, linperlisib, a novel oral PI3Kδ inhibitor, was evaluated as monotherapy for safety, tolerability and efficacy at recommended phase 2 dose of 80mg once daily. The clinical data from an interim data cutoff was presented at ASCO (Free ASCO Whitepaper) by Dr. Jie Jin, professor of First Hospital Affiliated with Zhe Jiang Medical University. Top line data from this study indicated that for the 38 r/r PTCL patients enrolled, 30 were evaluable. As of the data cutoff, an Overall Response Rate (ORR) of 70% was reported of which 33% were complete responses. A 100% disease control rate was also observed. Linperlisib was well-tolerated with Grade 1 and Grade 2 adverse events most frequently observed, and with limited Grade 3 adverse events of neutrophil decrease in 4 pts, (10.5%), and 1 (2.6%) case each of leukopenia, thrombocytopenia, blood lipase increase, pneumonia and stomatitis.

"Peripheral T cell lymphoma is a devastating and aggressive lymphoma where patients have very few treatment options in the relapsed and refractory setting," said Dr. Jie Jin. "The results of this Phase1b clinical trial suggest that linperlisib is a promising PI3Kδ selective inhibitor with important anti-tumor properties in this indication, and we hope it will be able to bring clinical benefits of linerlisib to patients suffering from this serious disease. Globally, there are no PI3K inhibitors that have been approved for the treatment of T cell lymphomas. In China, no PI3K inhibitors have been approved for any indications. By evaluating linperlisib for its safety, tolerability and efficacy, we are optimistic that this novel oral therapy will advance into registration clinical trials in PTCL for regulatory approval."

Linperlisib evaluated in advanced solid tumors

Another clinical study of linperlisib was also presented at ASCO (Free ASCO Whitepaper) entitled "A phase Ib study of the PI3Kδ inhibitor linperlisib in patients with advanced solid tumors". In this study that enrolled 78 advanced solid tumor patients, linperlisib monotherapy was evaluated for safety, tolerability, and durability at the recommended phase2 dose of 80 mg once daily, the dose previously established for the treatment of lymphomas. The clinical data from an interim analysis of this study was presented by Dr. Jin Li, Professor and Oncologist at Shanghai East Hospital.

Linperlisib is an immunomodulatory PI3Kδ inhibitor in solid tumors that has been demonstrated to alter the tumor immune microenvironment in preclinical research. "These properties of solid tumors are a challenge for therapeutic intervention because the regulatory immune cells will frequently repress an anti-tumor immune response. Our hypothesis is that linperlisib will unleash the anti-tumor suppression in a beneficial manner for patient treatments", said Zusheng Xu, General Manager of Yingli Pharma.

In the open-label Phase 1b study including 15 advanced solid tumor types, linperlisib was demonstrated to be safe and well-tolerated. The most common treatment related adverse events were Grade 1 and Grade 2, with the Grade 3 TRAE of neutropenia (3.8%), diarrhea (2.6%), elevated γ-glutaminase (1.3%) and leukopenia (1.3%) observed. The disease control rate with linperlisib monotherapy was reported to be 41.4%, with one complete response observed in a patient with thymic carcinoma.

Dr. Jin Li stated "Linperlisib is a PI3K inhibitor with a distinct chemical structure highly selective to the δ isoform, compared to other PI3K inhibitors. The preliminary clinical findings are supportive of Linperlisib demonstrating a favorable safety profile with very limited off-target effects that have been associated with other PI3K inhibitors in the clinic. We were pleased to see that Linperlisib can be administered to patients with advanced solid tumors in a manner that is safe and well-tolerated. Linperlisib has great potential for combination therapies and additional indications in the future. We committed to investigating how this new PI3K inhibitor can improve the health condition of patients suffering from advanced solid tumors."

YL-13027, a novel and selective TGFβR1 inhibitor in a Phase 1 dose escalation study

A first-in-human clinical trial of YL-13027, an oral, potent, and selective TGFβR1 inhibitor, is being presented at the ASCO (Free ASCO Whitepaper) meeting, entitled "A phase I study of a TGF-β receptor I kinase inhibitor YL-13027 in patients with advanced solid tumors".

TGFβ signaling is known to be a driver contributing to the immunosuppressive properties of many solid tumors. In principle, agents that interfere with TGFβ signaling may be beneficial towards interrupting tumor progression and supplying additional targets for anti-cancer therapies. YL-13027 was developed as a potent small molecule inhibitor of TGFβR1, a tyrosine kinase, and has demonstrated anti-tumor efficacy in preclinical models. In this open-label phase1 dose escalation study, the initial safety evaluation of YL-13027 was presented. The most frequent treatment related adverse events in twelve patients who had completed Cycle 1 safety evaluation period as of the data cut, were the following (all Grades/≥Grade 3): γ-glutamyl transferase elevation (38.5%/7.7%), hemoglobin decrease (38.5%/0%), blood alkaline phosphatase elevation (23.1%/7.7%), AST (23.1%/0%), and blood phosphorus decrease (23.1%/0%). Of the 6 evaluable patients with advanced solid tumors treated as of the data cutoff date, 1 triple negative breast cancer patient had a confirmed Partial Response.

"In recent years, immunotherapy has gradually replaced chemotherapy and radiotherapy, and has shown good clinical results for different types of advanced solid tumors, but we still encounter bottlenecks in terms of safety, tolerability and tumor indication selection” said Dr. Jin Li, professor of Shanghai East Hospital, and a lead investigator on the study. "YL-13027 has demonstrated to be a safe and tolerable oral agent that is highly selective for TGFβR1 over TGFβR2. These results are giving us confidence for the dose escalation of YL-13027, and its performance on other tumor types and combination therapies. We are very optimistic about the further development of YL-13027 as an anti-cancer agent."

Schedule for Linperlisib and YL-13027 presentations at ASCO (Free ASCO Whitepaper)

Abstract # 7531; ‘A phase Ib study of a PI3Kδ inhibitor Linperlisib in patients with relapsed or refractory peripheral T-cell lymphoma’ is being presented in the Hematologic Malignancies – Lymphoma and Chronic Lymphocytic Leukemia Session. Citation: J Clin Oncol 39, 2021 (suppl 15; abstr 7531)

Abstract # 3099; ‘A phase Ib study of the PI3Kδ inhibitor linperlisib in patients with advanced solid tumors’ is being presented in the Developmental Therapeutics – Molecularly Targeted Agents and Tumor Biology Session. Citation: J Clin Oncol 39, 2021 (suppl 15; abstr 3099)

Abstract # 3098; ‘A phase I study of a TGF-β receptor I kinase inhibitor YL-13027 in patients with advanced solid tumors’ is being presented in the Developmental Therapeutics – Molecularly Targeted Agents and Tumor Biology Session. Citation: J Clin Oncol 39, 2021 (suppl 15; abstr 3098)

About Linperlisib

Linperlisib (YY-20394) is a highly selective and potent PI3Kδ inhibitor that has shown favorable safety profile, exciting anti-tumor activities, and good PK and pharmaceutical properties as an oral once-a-day agent in late-stage clinical development. A phase 1 clinical trial was completed in 2020 demonstrating linperlisib to be a safe and tolerable agent, and a recommended phase 2 dose of 80 mg QD was established. Linperlisib received FDA Orphan Drug Designations for FL, CLL/SLL, and T cell lymphoma. Linperlisib was awarded NMPA Breakthrough Therapy status in China. A clinical trial in r/r FL for 93 patients having 2 or more prior systemic therapies has been completed and submitted for marketing approval in China. Additional linperlisib clinical trials are ongoing in other lymphomas, solid tumors, and in combination with gemcitabine/oxaliplatin in r/r DLBCL.

About YL-13027

YL-13027 is a potent small molecule antagonist of TGFβR1 kinase activity in early-stage clinical development. The compound was optimized with selectivity against TGFβR2 and other tyrosine kinases, differentiating YL-13027 from other inhibitors blocking TGFβ signaling. In preclinical studies, YL-13027 demonstrated anti-tumor efficacy and combination benefit with immunotherapy. In IND-enabling studies, YL-13027 showed reliable dose-proportionality and pharmacokinetic properties, and the agent proved to be safe and tolerable in toxicity studies. A phase 1 dose escalation of YL-13027 is continuing to establish a recommended phase2 dose of YL-13027.