TABLE 2.
Summary of approved small molecule nonkinase inhibitors
| Class | Drug name | Company | First approval | Targets | Administration pathway | Indications |
|---|---|---|---|---|---|---|
| HIF | Belzutifan (Welireg) | Merck | 2021 | HIF | Oral | VHL‐associated RCC, CNS hemangioblastomas and pNET |
| PARP | Olaparib (Lynparza) | AstraZeneca | 2014 | PARP1, PARP2, PARP3 | Oral | Ovarian, fallopian tube or primary peritoneal cancer, breast cancer, pancreatic cancer, prostate cancer |
| PARP | Rucaparib (Rubraca) | Clovis Oncology | 2016 | PARP1, PARP2, PARP3 | Oral | Ovarian cancer, prostate cancer |
| PARP | Niraparib (Zejula) | GlaxoSmithkline | 2017 | PARP1, PARP2 | Oral | Ovarian cancer |
| PARP | Talazoparib (Talzenna) | Pfizer | 2018 | PARP1, PARP2 | Oral | Breast cancer |
| DNMT | Azacitidine (Vidaza) | Celgene | 2004 | DNMT | Subcutaneous or intravenous | Myelodysplastic syndromes, AML, JMML |
| DNMT | Decitabine (Dacogen) | Otsuka | 2006 | DNMT | Intravenous | Myelodysplastic syndromes |
| HDAC | Vorinostat (Zolinza) | Merck | 2006 | HDAC1, HDAC2, HDAC3, HDAC6 | Oral | cutaneous T‐cell lymphoma |
| HDAC | Romidepsin (Istodax) | Celgene | 2010 | HDACs | Intravenous | Cutaneous T‐cell lymphoma |
| HDAC | Belinostat (Beleodaq) | Acrotech | 2014 | HDACs | Intravenous | Peripheral T‐cell lymphoma |
| HDAC | Panobinostat (Farydak) | Secura | 2015 | HDACs | Oral | Multiple myeloma |
| XPO1 | Selinexor (Xpovio) | Karyopharm Theraps | 2019 | XPO1 | Oral | Multiple myeloma, diffuse large B‐cell lymphoma |
| CXCR4 | Plerixafor (Mozobil) | Dr Reddys Labs | 2008 | CXCR4 | Subcutaneous | Autologous transplantation for NHL and MM |
| KRASG12C | Sotorasib (Lumakras) | Amgen | 2021 | KRASG12C | Oral | NSCLC with KRAS G12C‐mutation |
| mTOR | Temsirolimus (Torisel) | PF Prism CV | 2007 | mTOR | Intravenous | RCC |
| mTOR | Everolimus (Afinitor) | Novartis | 2009 | mTOR | Oral | HR‐positive, HER2‐negative breast cancer, neuroendocrine tumors, RCC, |
| mTOR | Sirolimus (albumin‐bound) (Fyarro) | DR Reddys Labs | 2021 | mTOR | Intravenous | Perivascular epithelioid cell tumor |
| SMO | Vismodegib (Erivedge) | GenenTech | 2012 | SMO | Oral | (Locally advanced)/metastatic basal cell carcinoma |
| SMO | Sonidegib (Odomzo) | Sun Pharm | 2015 | SMO | Oral | Local advanced basal cell carcinoma |
| SMO | Glasdegib (Daurismo) | Pfizer | 2018 | SMO | Oral | AML |
| BCL‐2 | Venetoclax (Venclexta) | Abbvie | 2016 | BCL‐2 | Oral | CLL/SLL, AML |
Abbreviations: RCC, renal cell carcinoma; pNET, pancreatic neuroendocrine tumor; NHL, non‐Hodgkin's lymphoma; MM, multiple myeloma; AML, acute myeloid leukemia; CLL/SLL, chronic lymphocytic leukemia/small lymphocytic lymphoma; JMML, juvenile myelomonocytic leukemia. Data sources: https://www.fda.gov/drugs/development‐approval‐process‐drugs/drug‐approvals‐and‐databases.