Small molecules make up over half of the 50 novel drugs approved by the FDA in 2021

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Written by

Ashley Moreno

Posted on

January 21, 2022

According to a recent article in Nature Reviews Drug Discovery, the Food and Drug Administration (FDA) in the US approved 50 novel therapeutics in 2021. 28 are small molecules (other than peptides and radiolabelled molecules). In this blog, we look at the newly approved therapeutics available in the Cambridge Structural Database (CSD).

Drug approvals in the US 2021

FDA drug approvals by type in 2021, Source: Nature Reviews Drug Discovery.


The overall approval count declined just slightly since the previous year. In 2020, the FDA’s Center for Drug Evaluation and Research (CDER) approved 53 new therapeutics, 38 of which were small molecules. Examples in the CSD from last year’s approvals are available here.

2021-approved drugs available in the CSD

In 2021, small molecules still accounted for over half of the total approvals. Five are currently available in the CSD. You can view all the structures below via WebCSD.


Rilpivirine is an HIV-1 antiviral. CSD refcode: OMAKOE01.

Structure of Rilpivirine


Dexmethylphenidate is an ADHD treatment. CSD refcode: YEGVIS.

Structure of dexmethylphenidate


Drospirenone is used in pregnancy prevention. CSD refcodes: XEZTON, XEZTON01, XEZTON02, XEZTON03.

Structure of drospirenone

Olanzapine and Samidorphan

Olanzapine is used in the treatment of schizophrenia and bipolar I disorder. CSD refcodes: UNOGIN, UNOGIN01, UNOGIN02, UNOGIN03, UNOGIN04, UNOGIN05.

Structure of olanzapine

Samidorphan is an HCl salt hydrate also used in the treatment of schizophrenia and bipolar I disorder. CSD refcode: XOSMOI.

Structure of samidorphan schizophrenia and bipolar disorder drug

Learn more

Read the whole article, “2021 FDA approvals” in Nature Reviews Drug Discovery.

Learn more about the CSD—the world’s repository for small-molecule organic and metal-organic crystal structures.

See how researchers around the world use Mercury—CCDC’s crystal structure visualization and exploration software—to advance structural science research.


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