AMG 319

Short description: Chemical compound

AMG 319

Clinical data
ATC code|

* None

Legal status
Legal status|

* Investigational

Identifiers

IUPAC name

* (S)-N-(1-[7-Fluoro-2-(pyridin-2-yl)quinolin-3-yl]ethyl)-9H-purin-6-amine

CAS Number|

* 1608125-21-8 Y

PubChem CID|

* 68947304

ChemSpider|

* 35000181

UNII|

* 19DG7G1U5Q

Chemical and physical data
Formula| C21H16FN7
Molar mass| 385.396 g·mol−1
3D model (JSmol)|

* Interactive image

SMILES

* C[C@@H](c1cc2ccc(cc2nc1c3ccccn3)F)Nc4c5c([nH]cn5)ncn4

InChI

* InChI=1S/C21H16FN7/c1-12(28-21-19-20(25-10-24-19)26-11-27-21)15-8-13-5-6-14(22)9-17(13)29-18(15)16-4-2-3-7-23-16/h2-12H,1H3,(H2,24,25,26,27,28)/t12-/m0/s1

* Key:KWRYMZHCQIOOEB-LBPRGKRZSA-N

AMG 319 is a drug developed by Amgen which acts as an inhibitor of the phosphoinositide 3-kinase enzyme subtype PI3Kδ. It was originally developed as an anti-inflammatory drug with potential applications in the treatment of autoimmune conditions such as rheumatoid arthritis, but subsequent research showed that it inhibits cell proliferation and might potentially have useful anti-cancer effects, and it has been put into clinical trials to assess its safety and tolerability in this application.[1][2]

## Contents

* 1 Mechanism(s) of action
* 2 Clinical trials
* 3 See also
* 4 References

## Mechanism(s) of action

It is a potential immunotherapy because blocking PI3Kδ (PI3K p110δ) eliminates a group of inhibitory immune cells and may allow the immune system to better attack the cancer cells.[3] p110δ inactivation in regulatory T cells unleashes CD8+ cytotoxic T cells.[4]

## Clinical trials

Its first clinical trial was a phase I/II study in adults with relapsed or refractory lymphoid malignancies.[5] This was due to run from 2011 to 2013.[citation needed]

In 2015/16 it started a phase II clinical trial as a neoadjuvant therapy for human papillomavirus (HPV) negative head and neck squamous-cell carcinoma (HNSCC) (prior to resection surgery).[3]

## See also

* Duvelisib
* Idelalisib

## References

1. ↑ "Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease". Journal of Medicinal Chemistry 58 (1): 480–511. January 2015. doi:10.1021/jm501624r. PMID 25469863.
2. ↑ "First-In-Human Study Of AMG 319, a Highly Selective, Small Molecule Inhibitor Of PI3Kδ, In Adult Patients With Relapsed Or Refractory Lymphoid Malignancies.". 55th ASH Annual Meeting and Exposition. December 2013. https://ash.confex.com/ash/2013/webprogram/Paper57332.html.
3. ↑ 3.0 3.1 Clinical trial number NCT02540928 for "AMG 319 in Human PapillomaVirus (HPV) Negative HNSCC" at ClinicalTrials.gov
4. ↑ "Inactivation of PI(3)K p110δ breaks regulatory T-cell-mediated immune tolerance to cancer". Nature 510 (7505): 407–411. June 2014. doi:10.1038/nature13444. PMID 24919154. Bibcode: 2014Natur.510..407A.
5. ↑ Clinical trial number NCT01300026 for "A Phase 1, First-in-Human Study Evaluating the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of AMG 319 in Adult Subjects With Relapsed or Refractory Lymphoid Malignancies" at ClinicalTrials.gov

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*[CID]: Compound ID