<?xml version="1.0"?>
<ownershipDocument>

    <schemaVersion>X0306</schemaVersion>

    <documentType>4</documentType>

    <periodOfReport>2017-09-19</periodOfReport>

    <issuer>
        <issuerCik>0001069308</issuerCik>
        <issuerName>Acer Therapeutics Inc.</issuerName>
        <issuerTradingSymbol>ACER</issuerTradingSymbol>
    </issuer>

    <reportingOwner>
        <reportingOwnerId>
            <rptOwnerCik>0001533139</rptOwnerCik>
            <rptOwnerName>PALMIN HARRY S</rptOwnerName>
        </reportingOwnerId>
        <reportingOwnerAddress>
            <rptOwnerStreet1>222 THIRD STREET</rptOwnerStreet1>
            <rptOwnerStreet2>SUITE #2240</rptOwnerStreet2>
            <rptOwnerCity>CAMBRIDGE</rptOwnerCity>
            <rptOwnerState>MA</rptOwnerState>
            <rptOwnerZipCode>02142</rptOwnerZipCode>
            <rptOwnerStateDescription></rptOwnerStateDescription>
        </reportingOwnerAddress>
        <reportingOwnerRelationship>
            <isOfficer>true</isOfficer>
            <officerTitle>Chief Financial Officer</officerTitle>
        </reportingOwnerRelationship>
    </reportingOwner>

    <nonDerivativeTable>
        <nonDerivativeTransaction>
            <securityTitle>
                <value>Common Stock</value>
            </securityTitle>
            <transactionDate>
                <value>2017-09-19</value>
            </transactionDate>
            <transactionCoding>
                <transactionFormType>4</transactionFormType>
                <transactionCode>J</transactionCode>
                <equitySwapInvolved>false</equitySwapInvolved>
                <footnoteId id="F1"/>
            </transactionCoding>
            <transactionAmounts>
                <transactionShares>
                    <value>125000</value>
                </transactionShares>
                <transactionPricePerShare>
                    <footnoteId id="F1"/>
                </transactionPricePerShare>
                <transactionAcquiredDisposedCode>
                    <value>A</value>
                </transactionAcquiredDisposedCode>
            </transactionAmounts>
            <postTransactionAmounts>
                <sharesOwnedFollowingTransaction>
                    <value>125000</value>
                </sharesOwnedFollowingTransaction>
            </postTransactionAmounts>
            <ownershipNature>
                <directOrIndirectOwnership>
                    <value>D</value>
                </directOrIndirectOwnership>
            </ownershipNature>
        </nonDerivativeTransaction>
    </nonDerivativeTable>

    <footnotes>
        <footnote id="F1">Received in connection with the Issuer's business combination (the &quot;Merger&quot;) with what was then known as &quot;Acer Therapeutics Inc.&quot; (&quot;Private Acer&quot;) in accordance with the terms of the Agreement and Plan of Merger and Reorganization dated June 30, 2017 among the Issuer, Opexa Merger Sub, Inc. and Private Acer, in exchange for 125,000 shares of common stock of Private Acer.</footnote>
    </footnotes>

    <ownerSignature>
        <signatureName>/s/ Daniel S. Clevenger, Attorney-in-Fact for Harry Palmin</signatureName>
        <signatureDate>2017-09-21</signatureDate>
    </ownerSignature>
</ownershipDocument>
