Drug Discovery and Development

  • Home Drug Discovery and Development
  • Drug Discovery
  • Women in Pharma and Biotech
  • Oncology
  • Neurological Disease
  • Infectious Disease
  • Resources
    • Video features
    • Podcast
    • Voices
    • Views
    • Webinars
  • Pharma 50
    • 2025 Pharma 50
    • 2024 Pharma 50
    • 2023 Pharma 50
    • 2022 Pharma 50
    • 2021 Pharma 50
  • Advertise
  • SUBSCRIBE

Olema Oncology’s OP-1250 could be a game-changing breast cancer drug

By Brian Buntz | July 29, 2022

Olema OncologyClinical-stage biopharma Olema Oncology’s (Nasdaq:OLMA) lead product candidate is OP-1250, an orally-available small molecule that recently won FDA Fast Track Designation for the treatment of ER+/HER2– metastatic breast cancer.

OP-1250 is a complete estrogen receptor antagonist with combined activity as a complete estrogen receptor (ER) antagonist (CERAN) and a selective ER degrader (SERD).

The drug candidate competes with estrogen for binding to the estrogen receptor to ensure it remains in an inactive state. It thus differs from drugs such as tamoxifen that do not completely inactivate the receptor.

The Fast Track Designation specifically covers human epidermal growth factor receptor 2-negative (HER2-) metastatic breast cancer that has progressed after patients receive at least one line of endocrine therapy. In addition, patients should receive at least one line of therapy with a cyclin-dependent kinase (CDK) 4/6 inhibitor.

Cyrus Harmon

Cyrus Harmon

Tens of thousands of U.S. patients meet that criteria every year, said Cyrus Harmon, co-founder and chief technology officer of Olema Oncology.

Potential broad opportunity for breast cancer in the long-run

For decades, scientists have known that the estrogen receptor is an important protein in the progression of estrogen-receptor-positive breast cancer.

OP-1250 could thus eventually find use in a larger number of breast cancer patients. “The broad opportunity is for all estrogen-receptor-positive breast cancers,” Harmon said in a recent interview. “OP-1250 has broad potential to be used throughout the spectrum of ER-positive breast cancer.”

Assuming the drug candidate ultimately wins FDA approval as a second-line therapy for ER+/HER2– breast cancer patients, Olema Oncology plans on continuing OP-1250 in clinical trials, comparing it to other standard-of-care treatments.

“There’s certainly potential for the drug to move into earlier settings down the road as well,” Harmon said.

There is historical precedent for endocrine agents for ER-positive breast cancer winning approval and then finding wider use over time. For instance, tamoxifen and FDA-approved aromatase inhibitors have eventually won authorization for adjuvant use in early breast cancer.

OP-1250 is now in a Phase 1/2 study and a Phase 1b study that is testing the drug candidate with Ibrance (palbociclib), which selectively inhibits CDK4 and CDK6.

In June, San Francisco–headquartered Olema announced a clinical trial update for OP-1250. The study found that it offered favorable tolerability and PK when paired with the CDK4/6 inhibitor palbociclib across initial dose escalation cohorts. In addition, there were no dose-limiting toxicities and no induced metabolism of palbociclib.

The company is planning on launching a pivotal monotherapy study in 2023.

Where OP-1250 fits into the breast cancer treatment landscape

While current breast cancer drugs such as tamoxifen, fulvestrant and aromatase inhibitors have their place, they have limitations. “We think OP-1250 may improve on each of those drugs in material ways,” Harmon said.

The emergence of activating mutations in the estrogen receptor is one of the primary mechanisms of resistance to aromatase inhibitors and the estrogen-receptor antagonist fulvestrant. “When that happens, the aromatase inhibitors don’t work as well because the receptor is active without estrogen, and fulvestrant doesn’t work as well because you need more drug to counter the action of the mutant receptor.”

The emergence of CDK 4/6 inhibitors such as abemaciclib (Verzenio), palbociclib (Ibrance) and ribociclib (Kisqali), when combined with endocrine therapy, has led to benefits in terms of progression-free survival and overall survival in hormone receptor-positive, HER2-negative metastatic breast cancers.

“OP-1250 has great potential both as monotherapy and as the preferred combination partner with other targeted therapies for ER-positive breast cancer,” Harmon said.


Filed Under: clinical trials, Drug Discovery, Oncology
Tagged With: ER, estrogen receptor, Olema Oncology, OP-1250
 

About The Author

Brian Buntz

As the pharma and biotech editor at WTWH Media, Brian has almost two decades of experience in B2B media, with a focus on healthcare and technology. While he has long maintained a keen interest in AI, more recently Brian has made making data analysis a central focus, and is exploring tools ranging from NLP and clustering to predictive analytics.

Throughout his 18-year tenure, Brian has covered an array of life science topics, including clinical trials, medical devices, and drug discovery and development. Prior to WTWH, he held the title of content director at Informa, where he focused on topics such as connected devices, cybersecurity, AI and Industry 4.0. A dedicated decade at UBM saw Brian providing in-depth coverage of the medical device sector. Engage with Brian on LinkedIn or drop him an email at bbuntz@wtwhmedia.com.

Related Articles Read More >

New treatment paradigms in oncology: Highlights from the ASCO 2025 annual meeting
Korean team reports all-in-one cancer nanomedicine in pre-clinical studies
As some biotechs cut, Genmab unveils striking new site near Princeton
OS Therapies announces favorable FDA feedback on external control arm strategy for osteosarcoma drug
“ddd
EXPAND YOUR KNOWLEDGE AND STAY CONNECTED
Get the latest news and trends happening now in the drug discovery and development industry.

MEDTECH 100 INDEX

Medtech 100 logo
Market Summary > Current Price
The MedTech 100 is a financial index calculated using the BIG100 companies covered in Medical Design and Outsourcing.
Drug Discovery and Development
  • MassDevice
  • DeviceTalks
  • Medtech100 Index
  • Medical Design Sourcing
  • Medical Design & Outsourcing
  • Medical Tubing + Extrusion
  • Subscribe to our E-Newsletter
  • Contact Us
  • About Us
  • R&D World
  • Drug Delivery Business News
  • Pharmaceutical Processing World

Copyright © 2025 WTWH Media LLC. All Rights Reserved. The material on this site may not be reproduced, distributed, transmitted, cached or otherwise used, except with the prior written permission of WTWH Media
Privacy Policy | Advertising | About Us

Search Drug Discovery & Development

  • Home Drug Discovery and Development
  • Drug Discovery
  • Women in Pharma and Biotech
  • Oncology
  • Neurological Disease
  • Infectious Disease
  • Resources
    • Video features
    • Podcast
    • Voices
    • Views
    • Webinars
  • Pharma 50
    • 2025 Pharma 50
    • 2024 Pharma 50
    • 2023 Pharma 50
    • 2022 Pharma 50
    • 2021 Pharma 50
  • Advertise
  • SUBSCRIBE