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# Immune checkpoint inhibitors

Antibodies that release the brakes on T cells (PD-1, PD-L1, CTLA-4) so the immune system attacks the cancer; the price is autoimmune-type side effects.

Updated Nov 1, 2026

## What they are

Intravenous antibodies against PD-1 (pembrolizumab, nivolumab, cemiplimab), PD-L1 (atezolizumab) and CTLA-4 (ipilimumab). They are used in melanoma, lung cancer, kidney cancer, head and neck cancer, Hodgkin lymphoma and tumours with mismatch-repair deficiency, among others.

## Mechanism of action

T cells carry inhibitory receptors that normally prevent autoimmunity. Tumours exploit them: PD-L1 on tumour cells switches off PD-1-positive T cells inside the tumour, and CTLA-4 limits T-cell priming in lymph nodes. Blocking these checkpoints lets T cells stay active and kill tumour cells, but it can also break tolerance to normal tissues.

Target: T-cell checkpoints PD-1, PD-L1 and CTLA-4

## Key points

- Immune-related adverse events can hit any organ: skin (rash, itching, vitiligo), colon (diarrhoea, colitis), liver (hepatitis), lung (pneumonitis), glands (thyroiditis, hypophysitis, adrenal insufficiency, type 1 diabetes), kidney, nerves and heart.
- Moderate to severe reactions: the drug is withheld and systemic corticosteroids are given; severe ones lead to permanent discontinuation.
- Anti-CTLA-4 (ipilimumab) causes more immune toxicity than anti-PD-1; the ipilimumab–nivolumab combination causes the most, including rare fatal myocarditis.
- Thyroid function, liver tests, glucose and creatinine are checked before each cycle.
- Responses can take months and tumours may look bigger at first because of inflammation.

## Drugs in this class

- [**Pembrolizumab** An anti-PD-1 antibody that reactivates T cells against many cancers, including melanoma, lung cancer and any tumour… Programmed cell death protein 1 (PD-1) on T cells](https://durgical.com/en/pharmacology/pembrolizumab/)
- [**Nivolumab** An anti-PD-1 antibody used in melanoma, lung, kidney, head and neck and liver cancer and Hodgkin lymphoma, alone or… Programmed cell death protein 1 (PD-1) on T cells](https://durgical.com/en/pharmacology/nivolumab/)
- [**Ipilimumab** Anti-CTLA-4 antibody for melanoma, often with nivolumab. It causes more immune toxicity (colitis, hypophysitis) than… Cytotoxic T-lymphocyte antigen 4 (CTLA-4)](https://durgical.com/en/pharmacology/ipilimumab/)
- [**Atezolizumab** An anti-PD-L1 antibody for lung cancer (including small cell), liver cancer with bevacizumab, and melanoma; adverse… Programmed death-ligand 1 (PD-L1) on tumour and immune cells](https://durgical.com/en/pharmacology/atezolizumab/)
- [**Cemiplimab** An anti-PD-1 antibody for advanced cutaneous squamous cell carcinoma, basal cell carcinoma after hedgehog inhibitors… Programmed cell death protein 1 (PD-1) on T cells](https://durgical.com/en/pharmacology/cemiplimab/)
- [**Nivolumab/relatlimab** Two checkpoint antibodies in one infusion: nivolumab blocks PD-1, relatlimab blocks LAG-3. Used in advanced melanoma… PD-1 (nivolumab) and LAG-3 (relatlimab) on T cells](https://durgical.com/en/pharmacology/nivolumab-relatlimab/)
- [**Durvalumab** Human anti-PD-L1 antibody that releases the brake on T cells. For lung, bladder, biliary, liver and other cancers… Programmed death-ligand 1 (PD-L1) on tumour and immune cells](https://durgical.com/en/pharmacology/durvalumab/)

## Others in the class

- durvalumab
- avelumab
- dostarlimab
- tremelimumab

## Test yourself

Think of the answer, then tap the question to see it.

## A patient on pembrolizumab develops several watery stools a day with abdominal pain. What is the likely cause and the key treatment?

Immune-mediated colitis; the drug is withheld and systemic corticosteroids are started according to severity.

## Where does CTLA-4 blockade act, compared with PD-1 blockade?

CTLA-4 blockade boosts T-cell priming in lymph nodes; PD-1/PD-L1 blockade reactivates T cells inside the tumour.

## Which endocrine problems should be looked for during checkpoint inhibitor treatment?

Hypo- or hyperthyroidism, hypophysitis, adrenal insufficiency and type 1 diabetes.

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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [Pembrolizumab Injection: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a614048.html) (MedlinePlus (U.S. National Library of Medicine), 2025); [Ipilimumab Injection: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a611023.html) (MedlinePlus (U.S. National Library of Medicine), 2023); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=L01FF) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.

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License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/classes/immune-checkpoint-inhibitors/
