FDA-Approved Drug Repurposing Libraries for Cancer Research

Cancer researchers face a persistent dilemma: de novo drug discovery demands multi-million-compound libraries, specialized screening infrastructure, long timelines, and substantial cost, while regulatory expectations around drug safety and efficacy continue to grow more complex. Against this backdrop, approved and clinical-phase compounds offer a lower-risk entry point into drug discovery, since they already carry documented bioactivity, safety, and bioavailability profiles. TargetMol addresses this need by supplying curated, annotated, and quality-validated compound libraries built specifically for drug repurposing, target identification, and high throughput or high content screening across oncology and related disease areas.

Why FDA-Approved Drug Repurposing Matters for Oncology

Repurposing approved drugs for new cancer indications shortens the path between hit identification and translational relevance, because the compounds involved have already passed through regulatory review or clinical trial phases. Rather than building a screening library from scratch, research teams can draw on compound sets where bioactivity, safety, and bioavailability are already characterized. TargetMol’s compound library portfolio was designed around exactly this logic, offering ready-to-screen collections annotated with structure, target, activity, IC50 value, and biological activity description so that screening hits can be interpreted quickly.

TargetMol’s FDA-Approved Drug Library

The L4200 FDA-Approved Drug Library is a core resource within TargetMol’s screening library offering, comprising 2,073 FDA-approved drugs assembled for high throughput screening (HTS) and high content screening (HCS). Each compound in this collection has bioactivity and safety confirmed through research evidence and clinical trials, which lowers the risk associated with uncharacterized compounds. The library spans oncology, cardiology, anti-inflammatory, immunology, neuropsychiatry, and analgesia research, making it a practical tool for discovering new uses for existing drugs and identifying new drug targets. Compounds are structurally diverse, medicinally active, and cell permeable, supporting cellular assay applications, and purity is validated through NMR and HPLC/LCMS testing.

Drug Repurposing Compound Library: Broader Regulatory and Target Coverage

For teams seeking a wider net, the L9200 Drug Repurposing Compound Library contains 5,745 approved and clinical drugs sourced with established regulatory pedigree—approved by FDA, EMA, or NMPA, or listed in USP, BP, EP, JP, or CP dictionaries. This collection covers targets such as 5-HT Receptor, Sodium Channel, p38 MAPK, PI3K, and MEK, and supports research across cancer, cardiovascular disease, immunology, and respiratory system applications. Compound annotation includes structure, target, activity, and a brief introduction, while NMR and HPLC testing confirms purity and quality.

Cancer-Focused Compound Collections

Beyond general-purpose repurposing libraries, TargetMol maintains several cancer-specific compound collections within its anti-cancer compound library series.

The L2110 Anti-Cancer Approved Drug Library includes 2,020 approved anti-cancer drugs selected from published literature and databases, intended for use as positive controls in biological cancer investigation and cancer correlation study. These compounds carry FDA, EMA, or NMPA approval along with annotated bioactivity, safety, and bioavailability, and the collection covers targets including PI3K, HDAC, mTOR, CDK, Aurora Kinase, and JAK, alongside disease areas such as lung cancer, breast cancer, leukemia, and lymphoma.

The L2150 Anti-Cancer Drug Library takes a combined approach, bringing together 3,755 drugs with demonstrated or potential anticancer activity from both FDA-approved and clinical trial sources. This library spans 15 different cancer research areas, including lung cancer, breast cancer, leukemia, and lymphoma, and supports molecular mechanism studies of tumorigenesis as well as anti-tumor drug repositioning discovery. Bioactivity and safety for these compounds are profiled in preclinical and clinical settings.

For teams working on general oncology screening, the L1000 Approved Drug Library offers 3,170 approved drugs sourced from FDA, EMA, or NMPA, with disease and target coverage spanning cancer, cardiovascular disease, GPCR/G protein, neuroscience, membrane transporter/ion channel, microbiology and virology, immunology/inflammation, and tyrosine kinase/adaptors. Notably, compounds in this library have also been identified as able to functionally replace reprogramming transcription factors, enhancing iPSC generation efficiency when used alone or in combination—an added dimension for teams studying cancer cell reprogramming.

Researchers requiring the largest screening set for tumor biology can turn to the L2100 Anti-cancer compound library, which contains 10,240 compounds selected for anti-tumor activity targeting the metabolism, growth, invasion, and metastasis of tumor cells. This library covers targets such as PI3K, HDAC, mTOR, CDK, Aurora Kinase, and JAK, with bioactivity and safety profiled in preclinical and clinical research and trials.

Quality Assurance Across the Portfolio

A consistent thread across TargetMol’s compound library offerings is structure and purity validation using NMR, HPLC, and LCMS testing methods. This validation approach is applied across library families, giving research teams a consistent basis for comparing and combining different libraries within a single project. Every library discussed here includes documented annotation—structure, target, activity, IC50 value, and biological activity description—so that screening results can be interpreted with appropriate context rather than treated as isolated data points.

Positioning for Research Teams

TargetMol’s overall value proposition centers on accelerating hit identification and drug optimization by providing ready-to-screen libraries of characterized compounds. For cancer research specifically, this means research teams working on drug repurposing, new target identification, or combination screening can select from multiple complementary libraries: a broad FDA-approved set, a repurposing-focused collection with multi-agency regulatory coverage, and several cancer-specific libraries ranging from positive-control reference compounds to large-scale anti-tumor screening sets. Each library within TargetMol’s compound library system is annotated, quality-validated, and oriented toward reducing the preclinical uncertainty that typically accompanies de novo compound screening.

For laboratories evaluating FDA-approved drug repurposing options for cancer research, TargetMol’s screening library portfolio offers a structured starting point—combining regulatory-backed compound provenance, detailed biological annotation, and validated purity across libraries built specifically for oncology-focused drug repositioning and mechanism studies.

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TargetMol Chemicals Inc.