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Vibliome Therapeutics, LLC, has developed a new, systematic approach that enables the design of small molecule Type II kinase inhibitors with unique profiles and a high degree of selectivity

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About Vibliome

Kinases are key regulators of cell function that represent one of the largest and most functionally diverse gene families. There are over 500 kinase enzymes encoded by the human genome which control nearly all cellular functions by phosphorylating proteins and other molecules. Aberrations in these cell signaling pathways affect cell metabolism, division, activation, growth and death, and are hallmarks in the development of cancer as well as other chronic diseases. Kinase inhibitors have been shown to be effective in targeting these aberrant signaling mechanisms that drive disease progression, yet currently-approved inhibitors act against fewer than 40 kinase targets.

In contrast to target-driven high-throughput screening approaches, Vibliome employs a strategy that integrates early profiling of its Type II discovery library against a panel of more than 400 kinase targets. This approach provides a unique SAR database, containing more than 2,000 compounds, to enable the development of novel Type II kinase inhibitors.

Vibliome is focused on the design of Type II inhibitors that lock kinase targets in an inactive conformation. By analyzing these structures across the kinome, the company has been able to identify unique similarities and differences between kinases that help to tune in selectivity. This structure-guided approach, coupled with the company's novel, annotated Type II kinase inhibitor library, is ideally suited to support precision medicine approaches for cancer and other diseases where selective kinase targeting is needed. Vibliome works with a global network of collaborators to use this approach to develop better medicines for the patients who need them the most.


Target: PLK4 (Polo-like kinase 4)
Stage: Lead Optimization

Centrosomes are organizing centers comprised of a pair of microtubule-based structures termed centrioles, and accurate control of centrosome number is critical for the maintenance of genomic integrity. Centriole duplication is under the control of PLK4, an upstream regulator of centriole assembly. Amplifications in chromosome 17q23 are common in cancers, particularly in breast cancer, and lead to tumor development and progression. When the gene TRIM37 (located within 17q23) is amplified in these cancers, centrosomal material is depleted and inhibition of PLK4 is synthetically lethal. Vibliome is developing a PLK4 inhibitor to treat cancer patients with TRIM37 amplifications, which are found in 9% of breast cancers, 40% of neuroblastomas, and potentially other cancer types.

Target: RIPK2 (Receptor-interacting protein kinase 2)
Stage: Lead Optimization

Receptor-interacting protein kinase 2 (RIPK2, also known as RIP2) is associated with NF-κB activation and cell death. Activity of RIPK2 is essential for the bacteria-sensing receptors NOD1/2 inflammatory signaling pathway, inducing proinflammatory and antimicrobial responses, and RIPK2 inhibitors significantly inhibit the immune response of NOD1/2. Excessive activation of RIPK2 is involved in the development of inflammatory bowel disease and other chronic inflammatory conditions. RIPK2 can also signal through kinases that are commonly associated with cancer progression: MKK7 (MAP2K7), DNA-PKcs (PRKDC), RSK2 (RPS6KA3), MST4 (STK26), MEK2 (MAP2K2), and CSK (CSK). In particular, the RIPK2/MKK7/JNK/c-Myc signaling pathway appears to be important in the progression of late-stage prostate cancer. Vibliome is developing a RIPK2 inhibitor to treat inflammatory diseases and castration-resistant prostate cancer.

Our mission to develop new therapeutic options for patients is backed by Deerfield Management in New York, an investment management firm committed to advancing healthcare through investment, information and philanthropy. The Firm works across the healthcare ecosystem to connect people, capital, ideas and technology in bold, collaborative and inclusive ways.

Vibliome Careers

Vibliome does not currently have any open positions.

Vibliome News

Vibliome Therapeutics and AssayQuant Technologies, Inc. Establish Collaborative Relationship

August 2, 2022

Vibliome Therapeutics, LLC, and AssayQuant Technologies, Inc., announced today that they have entered into an agreement whereby AssayQuant will provide Vibliome access to their proprietary PhosphoSens® Technology.

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Vibliome Therapeutics Spins Off New Company, Raises Additional Funding

February 24, 2022

Vibliome Therapeutics, LLC, announced today that it has executed an Asset Sale and License Agreement with Beartooth Therapeutics, Inc., for two of its proprietary kinase inhibitor programs against undisclosed targets.

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Vibliome Therapeutics Expands Its Kinase Inhibitor Discovery Library

January 11, 2021

Vibliome Therapeutics, LLC, announced today that it has expanded its highly curated proprietary kinase inhibitor discovery library to more than 500 unique compounds. This library is built on a common chemotype the company is leveraging for the development of novel therapeutics targeting clinically relevant cell signaling pathways.

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Vibliome Therapeutics Closes First Tranche of Its $16 million Series A Financing Round to Advance Selective Kinase Inhibitor Technology for Oncology and Other Disease Applications

April 29, 2019

Vibliome Therapeutics, LLC, announced that it closed a $16mm Series A round of financing to advance its proprietary technology supporting the development of small molecule therapeutics targeting clinically-relevant signaling pathways. Deerfield Management was the sole investor in the Series A financing round and will be providing operational support.

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Vibliome Team

Board of Directors

Robert Goodwin, PhD

Chief Executive Officer

Jason Fuller, PhD

Deerfield Management

Cameron Wheeler, PhD

Deerfield Management


Gary A. Flynn, Ph.D.

Robert Goodwin, Ph.D.

345 Park Avenue South, New York, NY 10010