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Tyrosine Kinase Inhibitors (TKIs) — Clinical Trials UK

Find actively recruiting tyrosine kinase inhibitor clinical trials in the UK. Explore EGFR inhibitors, BCR-ABL blockers, VEGFR antagonists, ALK inhibitors, and next-generation kinase therapies being tested across oncology, haematology, and rare diseases.

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What Are Tyrosine Kinase Inhibitors?

Tyrosine kinase inhibitors (TKIs) are oral small-molecule drugs that block tyrosine kinases — enzymes that act as molecular switches controlling cell growth, division, and survival. In many cancers and blood disorders, mutations cause these kinases to become permanently "switched on," driving uncontrolled cell proliferation. TKIs bind to the kinase domain and switch them off, halting disease progression with remarkable precision. They were among the first truly targeted cancer therapies and remain one of the most actively studied drug classes in clinical trials worldwide.

Types of TKIs in Clinical Trials

BCR-ABL Inhibitors

Target the BCR-ABL fusion protein that drives chronic myeloid leukaemia (CML). From imatinib (the first TKI) to second- and third-generation drugs like dasatinib, nilotinib, and ponatinib. Trials focus on treatment-free remission, resistance mutations, and newly diagnosed patients.

EGFR Inhibitors

Block the epidermal growth factor receptor in non-small cell lung cancer, head and neck cancer, and colorectal cancer. First-gen (gefitinib, erlotinib) through third-gen (osimertinib) target specific EGFR mutations. Trials explore resistance mechanisms, combination strategies, and adjuvant use.

VEGFR Inhibitors

Target vascular endothelial growth factor receptors to block tumour blood vessel formation (angiogenesis). Studied in renal cell carcinoma, hepatocellular carcinoma, thyroid cancer, and soft tissue sarcomas. Examples: sunitinib, sorafenib, pazopanib, axitinib.

ALK & ROS1 Inhibitors

Target ALK and ROS1 gene rearrangements found in a subset of NSCLC patients. From crizotinib to next-gen lorlatinib, alectinib, and brigatinib. Trials focus on CNS penetration, resistance (G1202R mutation), and first-line superiority.

Multi-Kinase Inhibitors

Broad-spectrum TKIs that simultaneously target multiple kinase pathways. Useful when tumours depend on several signalling cascades. Examples: lenvatinib (VEGFR + FGFR + RET), cabozantinib (VEGFR + MET + AXL). Trials explore wider tumour applications and combination with immunotherapy.

Next-Generation Selective TKIs

Highly selective kinase inhibitors designed to overcome resistance and reduce off-target toxicity. Includes KRAS G12C inhibitors (sotorasib, adagrasib), RET inhibitors (selpercatinib, pralsetinib), NTRK inhibitors (larotrectinib, entrectinib), and FGFR inhibitors (erdafitinib, futibatinib).

Conditions Using TKIs in Trials

TKIs are investigated in trials across many disease areas. Select a condition to explore relevant trials:

🩸 Leukaemia (CML) 🫁 NSCLC 🫘 Renal Cell Carcinoma 🎗️ Breast Cancer 🦋 Thyroid Cancer 🫘 Liver Cancer 🫀 Colorectal Cancer 🎗️ Ovarian Cancer ⚫ Melanoma 🔴 Lymphoma 🧠 Glioblastoma 🫘 Pancreatic Cancer

FAQs About TKI Trials

What are tyrosine kinase inhibitors and how do they work?
Tyrosine kinase inhibitors (TKIs) are small-molecule drugs that block the action of tyrosine kinases — enzymes that play a key role in cell signalling, growth, and division. In many cancers and blood disorders, tyrosine kinases become overactive due to genetic mutations. TKIs bind to these enzymes and prevent them from sending the signals that drive disease progression.
What cancers are TKIs used to treat in clinical trials?
TKIs are studied in clinical trials for a wide range of cancers including chronic myeloid leukaemia (CML), non-small cell lung cancer (NSCLC), renal cell carcinoma, breast cancer, thyroid cancer, gastrointestinal stromal tumours (GIST), hepatocellular carcinoma, and ovarian cancer. Different TKIs target different kinases relevant to each cancer type.
Are TKI clinical trials only for cancer?
While most TKI trials focus on oncology, some explore non-cancer applications. For example, TKIs targeting VEGFR are being studied in age-related macular degeneration, and JAK inhibitors (a subclass) treat autoimmune conditions like rheumatoid arthritis and psoriasis. The field is expanding into fibrosis, inflammatory diseases, and rare genetic conditions.
What are the side effects of TKIs in clinical trials?
Side effects vary by specific TKI but commonly include fatigue, diarrhoea, nausea, skin rash, liver enzyme elevation, and hypertension. Some TKIs have specific toxicities — for example, VEGFR inhibitors can cause hand-foot syndrome and proteinuria, while BCR-ABL inhibitors may cause fluid retention and muscle cramps. Trial protocols include regular monitoring for these effects.

Related Treatment Types

🎯 Targeted Therapy

Broader precision treatments targeting specific molecular features of disease

💊 PARP Inhibitors

Targeted therapies exploiting DNA repair deficiencies in cancer cells

🧪 Antibody-Drug Conjugates

Precision delivery of potent drugs via antibody targeting

🔬 JAK Inhibitors

Related kinase inhibitors targeting the JAK-STAT inflammatory pathway

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