FLAG Therapeutics’ two novel classes of investigational drugs, Anti-angiogenic & Anti-tubulin (AA/AT) and Purine Synthesis Inhibitors (PSI), are designed to harness the power of multiple therapeutic actions targeted by highly water-soluble small molecule compounds.

Engineered to specifically overcome the shortcomings of conventional cancer therapies, namely efficacy, tolerability and drug resistance issues, FLAG’s investigational compounds hold the potential to treat multiple cancer types, including brain, lung, ovarian and pancreatic.  

To date, more than $25 million in non-dilutive funding has been used to synthesize, optimize and screen compounds in vitro and in vivo, resulting in a library of thousands of promising compounds. The mechanisms of action for both classes of compounds have been fully elucidated and validated, thereby potentially minimizing development risks and facilitating clinical development.

FLAG's compounds have undergone:

  • Structural Activity Relationship (SAR) Analysis

  • Molecular modeling

  • In vitro activity screening (NCI 60 cell line panel)

  • Mechanism of action elucidation

  • In vivo efficacy studies with clinically relevant comparator


Anti-angiogenic & Anti-tubulin (AA/AT)

FLAG’s lead candidate, FLAG-003, is a clinical-stage product under investigational use for Glioma.

FLAG’s AA/AT compounds are the only dual-acting small molecule compounds that combine the proven activity of the two primary classes of oncology therapeutics. 

These compounds are designed to circumvent the two major mechanisms of drug resistance (Pgp and β-III tubulin overexpression) that limit the utility of current cytotoxic therapies (such as taxanes and vinca alkaloids).

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Bi-specific, Single agent

Anti-angiogencic (blue) - Not a substrate for PGP or ß-III (and therefore shows no resistance mechanism) and binds specifically to EGFR, VEGF and PDGFR growth factors.

Anti-tubulin (red) - Inhibits tubulin assembly and suppresses microtubule formation at the colchicine binding site


Purine Synthesis Inhibitors (PSI)

FLAG’s Purine Synthesis Inhibitors (PSI) are novel compounds meticulously designed to avoid uptake by the ubiquitous RFC and to enter cells only via receptor sites that are over-expressed on cancer cells (e.g., folate receptor alpha, beta and PCFT), leaving normal cells intact.

purine synthesis inhibitor


PSI’s are designed to impart cytotoxicity via potent inhibition of β-glycinamide ribonucleotide formyltransferase (GARFTase), which catalyzes the first folate-dependent reaction in de novo purine nucleotide biosynthesis as well as inhibits one-carbon mitochondrial processing via SHMT-1 and SHMT-2 inhibition.


Strong Intellectual Property Portfolio

FLAG protects its product platforms through a strong intellectual property portfolio. Portfolio highlights currently include:

  • 63 issued patents

  • 56+ pending applications

  • Patents covering composition of matter and uses

  • Patent coverage extending beyond 2035 (including 7- to 10-year orphan drug designation extension)



February 2016: Granted Orphan Drug Designation (applied in October 2015) for FLAG-003 for the treatment of Glioma in both the US and EU.

October 2016: Hosted successful pre-IND meeting with US FDA.

September 2017: Awarded $1.5 M 2-year SBIR to study PSI molecules for the treatment of Mesothelioma.

Early 2019: Plans to file IND for a Phase I study of FLAG-003 for the treatment of Glioma.


Our Development Pipeline

FLAG's founded its pipeline upon promising research data generated in a variety of preclinical studies, investigator driven studies and FLAG-sponsored clinical trials.

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FLAG continues to advance oncological research. For a list of recent publications click here.